The control of invertebrate pests is extremely important in achieving high crop efficiency. Damage by invertebrate pests to growing and stored agronomic crops can cause significant reduction in productivity and thereby result in increased costs to the consumer.

The control of invertebrate pests in forestry, greenhouse crops, ornamentals, nursery crops, stored food and fiber products, livestock, household, and public and animal health is also important. Many products are commercially available for these purposes, but the need continues for new compounds that are more effective, less costly, less toxic, environmentally safer or have different modes of action.

WO 99/14202 discloses pyrimidin-4-one and pyrimidin-4-thiones of Formula i as fungicides wherein, inter alia, XisOorS ; A is fused phenyl or pyridyl; R1 and R are selected from H, halogen or trimethylsilyl; R3 is C1-Cg alkyl, C1-Cg alkenyl or C1-Cg alkynyl, each optionally substituted; and R4 is optionally substituted phenyl.

SUMMARY OF THE INVENTION This invention pertains to a method for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound of Formula I, its N-oxide or an agriculturally suitable salt of the compound (e. g., as a composition described herein)

wherein B is 0 or S ; J is a phenyl ring substituted with 1 to 4 R5, or a naphthyl ring system, a 5-or 6-membered heteroaromatic ring or an aromatic 8-, 9-or 10-membered fused heterobicyclic ring system wherein each ring or ring system is optionally substituted with 1 to 4 R5 ; K is, together with the two contiguous linking carbon atoms, a fused phenyl or a fused pyridinyl ring selected from the group consisting of K-1, K-2, K-3, IL-4 and K-5, each optionally substituted with 1 to 4 R4 R3 is G; C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C3-C6 cycloalkyl, each optionally substituted with one or more substituents selected from the group consisting of halogen, G, CN, NO2, hydroxy, C1-C4 alkoxy, C1-C4 haloalkoxy, C1-C4 alkylthio, Cl-C4 alkylsulfinyl, Cl-C4 alkylsulfonyl, C-Cg alkoxycarbonyl, C2-C6 alkylcarbonyl, C3-C6 trialkylsilyl, or a phenoxy ring optionally substituted with one to three substituents independently selected from R6 ; hydroxy; Cl-C4 alkoxy; Cl-C4 alkylamino; C2-C8 dialkylamino ; C3-C6 cycloalkylamino ; C2-C6 alkoxycarbonyl or C2-C6 alkylcarbonyl; G is a phenyl ring or 5-or 6-membered heteroaromatic ring, each ring optionally substituted with one to three substituents independently selected from R6 ; a 5-or 6-membered nonaromatic carbocyclic or heterocyclic ring, optionally including

one or two ring members selected from the group consisting of C (=O), SO or S (0) 2 and optionally substituted with 1 to 4 substituents selected from R12 ; each R4 is independently H, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C3-C6 cycloalkyl, Cl-C6 haloalkyl, C2-C6 haloalkenyl, C2-C6 haloalkynyl, C3-C6 halocycloalkyl, halogen, CN, NO2, hydroxy, Cl-C4 alkoxy, C1-C4 haloalkoxy, C1-C4 alkylthio, C1-C4 alkylsulfinyl, C1-C4 alkylsulfonyl, C1-C4 haloalkylthio, C1-C4 haloalkylsulfinyl, C1-C4 haloalkylsulfonyl, Cl-C4 alkylamino, C2-C8 dialkylamino, C3-C6 cycloalkylamino, Cl-C4 alkoxyalkyl, Cl-C4 hydroxyalkyl, C (O) Ri0, CO2Rl°, C (O) NR10R11, NR10R11, N(R11)COR10, N (R11)CO2R10 or C3-C6 trialkylsilyl; or each R4 is independently a phenyl, benzyl, phenoxy or a 5-or 6-membered heteroaromatic ring, each ring optionally substituted with one to three substituents independently selected from R6 ; each R5 is independently H, C1-C6 alkyl, Cl--C6 alkenyl, C2-C6 alkynyl, C3-C6 cycloalkyl, C1-C6 haloalkyl, C2-C6 haloalkenyl, C2-C6 haloalkynyl, C3-C6 halocycloalkyl, halogen, CN, CO2H, CONH2, NO,), hydroxy, C1-C4 alkoxy, Cl-C4 haloalkoxy, Cl-C4 alkylthio, C1-C4 alkylsulfinyl, Cl-C4 alkylsulfonyl, Cl-C4 haloalkylthio, Cl-C4 haloalkylsulfinyl, Cl-C4 haloalkylsulfonyl, C1-C4 alkylamino, Cy-Cg dialkylamino, C3-C6 cycloalkylamino, C2-C6 alkylcarbonyl, C2-C6 alkoxycarbonyl, C2-C6 alkylaminocarbonyl, C3-C8 dialkylaminocarbonyl, C3-C6 trialkylsilyl; or each R5 is independently a phenyl, benzyl, benzoyl, phenoxy, 5-or 6-membered heteroaromatic ring or an aromatic 8-, 9-or 10-membered fused heterobicyclic ring system, each ring optionally substituted with one to three substituents independently selected from R6 ; or (R5) 2 when attached to adjacent carbon atoms can be taken together as-OCF2O-, -CF2CFrO-, or-OCFCF20-; each R6 is independently C1-C4 alkyl, C2-C4 alkenyl, C2-C4 alkynyl, C3-C6 cycloalkyl, C1-C4 haloalkyl, C2-C4 haloalkenyl, C2-C4 haloalkynyl, C3-C6 halocycloalkyl, halogen, CN, NO2, C1-C4 alkoxy, C1-C4 haloalkoxy, Cl-C4 alkylthio, Cl-C4 alkylsulfinyl, Cl-C4 alkylsulfonyl, Cl-C4 alkylamino, C2-Cg dialkylamino, C3-C6 cycloalkylamino, C3-C6 (alkyl) cycloalkylamino, C2-C4 alkylcarbonyl, C2-C6 alkoxycarbonyl, C2-C6 alkylaminocarbonyl, C3-Cg dialkylaminocarbonyl or C3-C6 trialkylsilyl ; RIO is H or Ci-C4 alkyl or C1-C4 haloalkyl ; Rll is H or C1-C4 alkyl ; each Ri'is independently C1-C2 alkyl, halogen, CN, NO,) and C1-C2 alkoxy; and n is 1 to 4.

This invention also relates to such a method wherein the invertebrate pest or its environment is contacted with a biologically effective amount of a compound of Formula I or a composition comprising a compound of Formula I and a biologically effective amount of at least one additional compound or agent for controlling invertebrate pests.

This invention also pertains to a compound of Formula la, its N-oxide or an agriculturally suitable salt of the compound

la wherein K is, together with the two contiguous linking carbon atoms, a fused phenyl or a fused pyridinyl ring selected from the group consisting of K-1, K-2, K-3, K-4 and K-5, each optionally substituted with 1 to 4 R4 J substituted with 1 to 3 RS is selected from the group consisting of J-6, J-7, J-8, J-9, J-10, J-11, J-12 and J-13

R3 is C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl or C3-C6 cycloalkyl each optionally substituted with one or more substituents selected from the group consisting of halogen, CN, Cl-C2 alkoxy, C1-C2 alkylthio, C1-C2 alkylsulfinyl and Cl-C2 alkylsulfonyl ; one R4 group is attached to the K-ring at the 2-position or 5-position, and said R4 is C1-C4 alkyl, C1-C4 haloalkyl, halogen, CN, NO2, Cl-C4 alkoxy, Cl-C4 haloalkoxy, C1-C4 alkylthio, C1-C4 alkylsulfinyl, Cl-C4 alkylsulfonyl, C1-C4 haloalkylthio, C1-C4 haloalkylsulfinyl, or C1-C4 haloalkylsulfonyl ; and an optional second R4 is H, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C3-C6 cycloalkyl, C1-C6 haloalkyl, C2-C6 haloalkenyl, C2-C6 haloalkynyl, C3-C6 halocycloalkyl, halogen, CN, NO2, hydroxy, Cl-C4 alkoxy, Cl-C4 haloalkoxy, C1-C4 alkylthio, C1-C4 alkylsulfinyl, C1-C4 alkylsulfonyl, C1-C4 haloalkylthio, C1-C4 haloalkylsulfinyl, C1-C4 haloalkylsulfonyl, C1-C4 alkylamino, C2-C8 dialkylamino, C3-C6 cycloalkylamino, C1-C4 alkoxyalkyl, C1-C4 hydroxyalkyl, C (O) R10, CO2R10, C (O) NR10R11, NR10R11, N(R11)COR10, N (Rl') CO2R10 or C3-C6 trialkylsilyl; R5 is V is N, CH, CF, CCI, CBr or CI ; each R6 is independently Cl-C4 alkyl, C2-C4 alkenyl, C2-C4 alkynyl, C3-Cg cycloalkyl, Cl-C4 haloalkyl, C2-C4 haloalkenyl, C2-C4 haloalkynyl, C3-C6 halocycloalkyl, halogen, CN, NO, Cl-C4 alkoxy, C1-C4 haloalkoxy, C1-C4 alkylthio, C1-C4 alkylsulfinyl, C1-C4 alkylsulfonyl, C1-C4 alkylamino, C2-C8 dialkylamino, C3- C6 cycloalkylamino, C3-C6 (alkyl) cycloalkylamino, C2-C4 alkylcarbonyl, C2-C6 alkoxycarbonyl, C2-C6 alkylaminocarbonyl, C3-Cs dialkylaminocarbonyl or C3- C6 trialkylsilyl;

each R7 is independently H, C1-C6 alkyl, C1-C6 haloalkyl, halogen, CN, Cl-C4 alkoxy, C1-C4 haloalkoxy or C1-C4 haloalkylthio; R9 is H, C2-C6 alkyl, C1-C6 haloalkyl, C3-C6 alkenyl, C3-C6 haloalkenyl, C3-C6 alkynyl or C3-C6 haloalkynyl, provided that R7 and R9 are not both H; RIO is H or Ci-C4 alkyl or C1-C4 haloalkyl ; R11 is H or C1-C4 alkyl ; and n is 0, 1 or 2.

This invention also pertains to a composition for controlling an invertebrate pest comprising a biologically effective amount of a compound of Formula la and at least one additional component selected from the group consisting of surfactants, solid diluents and liquid diluents. This invention also pertains to a composition comprising a biologically effective amount of a compound of Formula la and an effective amount of at least one additional biologically active compound or agent.

DETAILS OF THE INVENTION In the above recitations, the term"alkyl", used either alone or in compound words such as"alkylthio"or"haloalkyl"includes straight-chain or branched alkyl, such as methyl, ethyl, n-propyl, i-propyl, or the different butyl, pentyl or hexyl isomers."Alkenyl"includes straight-chain or branched alkenes such as 1-propenyl, 2-propenyl, and the different butenyl, pentenyl and hexenyl isomers."Alkenyl"can also include polyenes such as 1, 2-propadienyl and 2,4-hexadienyl."Alkynyl"includes straight-chain or branched alkynes such as 1-propynyl, 2-propynyl and the different butynyl, pentynyl and hexynyl isomers."Alkynyl" can also include moieties comprised of multiple triple bonds such as 2,5-hexadiynyl.

"Alkoxy"includes, for example, methoxy, ethoxy, 7 ?-propyloxy, isopropyloxy and the different butoxy, pentoxy and hexyloxy isomers."Alkoxyalkyl"denotes alkoxy substitution on alkyl. Examples of"alkoxyalkyl"include CH3OCH2, CH30CHCH2, CH3CH2OCHo, CH3CH2CH2CH2OCH2 and CH3CH9OCHoCH2."Alkylthio"includes branched or straight-chain alkylthio moieties such as methylthio, ethylthio, and the different propylthio, butylthio, pentylthio and hexylthio isomers."Cycloalkyl"includes, for example, cyclopropyl, cyclobutyl, cyclopentyl and cyclohexyl.

The term"heteroaromatic ring"denotes fully aromatic rings in which at least one ring atom is not carbon and can contain 1 to 4 heteroatoms independently selected from the group consisting of nitrogen, oxygen and sulfur, provided that each heteroaromatic ring contains no more than 4 nitrogens, no more than 2 oxygens and no more than 2 sulfurs (where aromatic indicates that the Hiickel rule is satisfied). The heteroaromatic ring can be attached through any available carbon or nitrogen by replacement of hydrogen on said carbon or nitrogen.

The term"halogen", either alone or in compound words such as"haloalkyl", includes fluorine, chlorine, bromine or iodine. Further, when used in compound words such as "haloalkyl", said alkyl may be partially or fully substituted with halogen atoms which may

be the same or different. Examples of"haloalkyl"include F3C, CICH, CF3CH2 and CF3CC1o. The tenns"haloalkenyl","haloalkynyl","haloalkoxy", and the like, are defined analogously to the tenn"haloalkyl". Examples of"haloalkenyl"include (C1) 2C=CHCHo and CF3CH2CH=CHCH2. Examples of"haloalkynyl"include HC=CCHCI, CF3C=C, CC13C=-C and FCH2C=CCH2. Examples of"haloalkoxy"include CF30, CC13CH20, HCF2CH2CH20 and CF3CH20.

The total number of carbon atoms in a substituent group is indicated by the"Ci-Cj" prefix where i and j are numbers from 1 to 6. For example, Cl-C3 alkylsulfonyl designates methylsulfonyl through propylsulfonyl ; C2 alkoxyalkyl designates CH30CH2; C3 alkoxyalkyl designates, for example, CH3CH (OCH3), CH30CH2CH2 or CH3CH20CHo ; and C4 alkoxyalkyl designates the various isomers of an alkyl group substituted with an alkoxy group containing a total of four carbon atoms, examples including CH3CH2CH20CH2 and CH3CHrOCH2CH2. In the above recitations, when a compound of Formula 1 contains a heteroaromatic ring, all substituents are attached to this ring through any available carbon or nitrogen by replacement of a hydrogen on said carbon or nitrogen.

When a group contains a substituent which can be hydrogen, for example R3, then, when this substituent is taken as hydrogen, it is recognized that this is equivalent to said group being unsubstituted.

Compounds of this invention can exist as one or more stereoisomers. The various stereoisomers include enantiomers, diastereomers, atropisomers and geometric isomers. One skilled in the art will appreciate that one stereoisomer may be more active and/or may exhibit beneficial effects when enriched relative to the other stereoisomer (s) or when separated from the other stereoisomer (s). Additionally, the skilled artisan knows how to separate, enrich, and/or to selectively prepare said stereoisomers. Accordingly, the compounds of the invention may be present as a mixture of stereoisomers, individual stereoisomers, or as an optically active form.

The present invention comprises compounds selected from Formula I, N-oxides and agriculturally suitable salts thereof, compositions thereof and methods of their use for invertebrate pest control. One skilled in the art will appreciate that not all nitrogen containing heterocycles can form N-oxides since the nitrogen requires an available lone pair for oxidation to the oxide; one skilled in the art will recognize those nitrogen containing heterocycles which can form N-oxides. One skilled in the art will also recognize that tertiary amines can form N-oxides. Synthetic methods for the preparation of N-oxides of heterocycles and tertiary amines are very well known by one skilled in the art including the oxidation of heterocycles and tertiary amines with peroxy acids such as peracetic and m-chloroperbenzoic acid (MCPBA), hydrogen peroxide, alkyl hydroperoxides such as t-butyl liydroperoxide, sodium perborate, and dioxiranes such as dimethydioxirane. These methods for the preparation of N-oxides have been extensively described and reviewed in the

literature, see for example: T. L. Gilchrist in Comprehensive Organic Synthesis, vol. 7, pp 748-750, S. V. Ley, Ed., Pergamon Press; M. Tisler and B. Stanovnik in Comprehensive Hetenocyclic Cltemisty, vol. 3, pp 18-19, A. J. Boulton and A. McKillop, Eds., Pergamon Press; M. R. Grimmett and B. R. T. Keene in Advances in Heterocyclic Chemistry, vol. 43, pp 139-151, A. R. Katritzky, Ed., Academic Press; M. Tisler and B. Stanovnik in Advances in Heterocyclic Chemistry, vol. 9, pp 285-291, A. R. Katritzky and A. J. Boulton, Eds., Academic Press; and G. W. H. Cheeseman and E. S. G. Werstiuk in Advances in Heterocyclic Chemistry, vol. 22, pp 390-392, A. R. Katritzky and A. J. Boulton, Eds., Academic Press.

The salts of the compounds of the invention include acid-addition salts with inorganic or organic acids such as hydrobromic, hydrochloric, nitric, phosphoric, sulfuric, acetic, butyric, fumaric, lactic, maleic, malonic, oxalic, propionic, salicylic, tartaric, 4-toluenesulfonic or valeric acids.

Preferred methods for reasons of better activity, cost and/or ease of synthesis are: Preferred 1. Methods wherein for the compounds of Formula I B is O and R3 is Cl-C6 alkyl, Co-C6 alkenyl, C2-C6 alkynyl or C3-C6 cycloalkyl each optionally substituted with one or more substituents selected from the group consisting of halogen, CN, Cl-C2 alkoxy, Cl-C2 alkylthio, Cl-C2 alkylsulfinyl and Cl-C2 alkylsulfonyl.

Preferred 2. Methods of Preferred 1 wherein J is a phenyl group substituted with 1 to 4R5.

Preferred 3. Methods of Preferred 2 wherein n is 1 to 2; one R4 group is attached to the K-ring at the 2-position or 5-position, and said R4 is C1-C4 alkyl, C1-C4 haloalkyl, halogen, CN, NO2, Cl-C4 alkoxy, Cl-C4 haloalkoxy, Cl-C4 alkylthio, Cl-C4 alkylsulfinyl, Cl-C4 alkylsulfonyl, Cl-C4 haloalkylthio, Cl-C4 haloalkylsulfinyl or Cl-C4 haloalkylsulfonyl ; and each R5 is independently H, halogen, Cl-C4 alkyl, Cl-C2 alkoxy, Cl-C4 haloalkyl, CN, NO2, Cl-C4 haloalkoxy, Cl-C4 alkylthio, Cl-C4 alkylsulfinyl, Cl-C4 alkylsulfonyl, Cl-C4 haloalkylthio, Cl-C4 haloalkylsulfinyl, Cl-C4 haloalkylsulfonyl or C ?-C4 alkoxycarbonyl; or each R5 is independently a phenyl or a 5-or 6-membered heteroaromatic ring, each ring optionally substituted with R6 ; or (R5) 2 when attached to adjacent carbon atoms can be taken together as -OCF2O-, -CF2CF2O- or -OCF2CF2O-.

Preferred 4. Methods of Preferred 3 wherein

R3 is Cl-C4 alkyl optionally substituted with halogen, CN, OCH3 or S (O) pCH3; one R4 group is attached to the R-ring at the 2-position and said R4 is CH3, CF3, OCF3, OCHF, S(O) pCF3, S (O) pCHF2, CN or halogen; a second R4 is H, F, Cl, Br, I or CF3 ; each R5 is independently H, halogen, methyl, CF3, OCF3, OCHF2, S (O) pCF3, S (O) pCHF2, OCH2CF3, OCF2CHF2, S (O) pCH2CF3 or S (O) pCF2CHF2 ; or a phenyl, pyrazole, imidazole, triazole, pyridine or pyrimidine ring, each ring optionally substituted with C1-C4 alkyl, C1-C4 haloalkyl, halogen or CN; and pis0, 1 or2.

Preferred 5. Methods of Preferred 4 wherein R3 is i-propyl or t-butyl.

Preferred 6. Methods of Preferred 1 wherein J is a 5-or 6-membered heteroaromatic ring optionally substituted with 1 to 4 R5.

Preferred 7. Methods of Preferred 6 wherein J is a 5-or 6-membered heteroaromatic ring selected from the group consisting of J-1, J-2, J-3, J-4 and J-5, each J optionally substituted with 1 to 3 R5 Q is 0, S or NR5 ; and W, X, Y and Z are independently N or CR5, provided that in J-4 and J-5 at least one of W, X, Y or Z is N.

Preferred 8. Methods of Preferred 7 wherein n is 1 to 2 ; one R4 group is attached to the Is-ring at the 2-position or 5-position, and said R4 is C1-C4 alkyl, Cl-C4 haloalkyl, halogen, CN, N02, Cl-C4 alkoxy, C1-C4 haloalkoxy, C1-C4 alkylthio, C1-C4 alkylsulfinyl, C1-C4 alkylsulfonyl, Cl-C4 haloalkylthio, Ci-C4 haloalkylsulfinyl, or C1-C4 haloalkylsulfonyl ; and each R5 is independently H, Cl-C4 alkyl, Cl-C4 haloalkyl, halogen, CN, NO2, Cl-C4 haloalkoxy, Cl-C4 alkylthio, Cl-C4 alkylsulfinyl, Cl-C4 alkylsulfonyl, Cl-C4 haloalkylthio, Ci-C4 haloalkylsulfinyl, C1-C4 haloalkylsulfonyl or C2-C4 alkoxycarbonyl; or a phenyl or a 5-or

6-membered heteroaromatic ring, each ring optionally substituted with R6.

Preferred 9. Methods of Preferred 8 wherein J substituted with 1 to 3 R5 is selected from the group consisting of J-6, J-7, J-8, J-9, J-10, J-l 1, J-12 and J-13 V is N, CH, CF, CCI. CBr or CI ; each R7 is independently H, C1-C6 alkyl, C1-C6 haloalkyl, halogen, CN, Cl-C4 alkoxy, Cl-C4 haloalkoxy or Cl-C4 haloalkylthio; R9 is H, C2-C6 alkyl, Cl-C6 haloalkyl, C3-C6 alkenyl, C3-C6 haloalkenyl, C3-C6 alkynyl or C3-C6 haloalkynyl, provided that R7 and R9 are not both H; and n is 0, 1 or 2.

Preferred 10. Methods of Preferred 9 wherein J substituted with 1 to 3 R5 is J-6; R3 is C1-C4 alkyl optionally substituted with halogen, CN, OCH3, S (O) pCH3 ; one R4 group is attached to the K-ring at the 2-position and said R4 is CH3, CF3, OCF3, OCHF2, S (O) pCF3, S (O) pCHF2, CN or halogen;

a second R4 is H, F, Cl, Br, I or CF3; R6 is C1-C4 alkyl, Cl-C4 haloalkyl, halogen or CN; R7 is CH3, CF3, OCHF2 or halogen ; and pis0, 1 or2.

Preferred 11. Methods of Preferred 10 wherein R3 is C1-C4 alkyl ; one R4 group is attached to the K-ring at the 2-position and said R4 is CH3, Cl or Br ; a second R4 is H, F, Cl, Br, I or CF3 ; R6 is Cl or Br; and R7 is halogen or CF3.

Preferred 12. Methods of Preferred 9 wherein J substituted with I to 3 R5 is J-7; R3 is Cl-C4 alkyl optionally substituted with halogen, CN, OCH3, S (O) pCH3; one R4 group is attached to the K-ring at the 2-position and said R4 is CH3, CF3, OCF3, OCHF, S (O) pCF3, S (O) pCHF2, CN or halogen; a second R4 is H, F, Cl, Br, I or CF3; R6 is C1-C4 alkyl, C1-C4 haloalkyl, halogen or CN; R9 is C2-C6 alkyl or Cl-C6 haloalkyl ; and p is 0, 1 or 2.

Preferred 13. Methods of Preferred 12 wherein R3 is C1-C4 alkyl ; one R4 group is attached to the K-ring at the 2-position and said R4 is CH3, Cl or Br ; a second R4 is H, F, Cl, Br, I or CF3; R6 is Cl or Br; and R9 is CF3, CHF2, CBrF2, CCIF9, CHCF3, or CF2CHF2.

Preferred 14. Methods of Preferred 9 wherein J substituted with 1 to 3 R5 is J-S ; R3 is Cl-C4 alkyl optionally substituted with halogen, CN, OCH3, S (O) pCH3; one R4 group is attached to the K-ring at the 2-position and said R4 is CH3, CF3, OCF3, OCHF2, S (O) pCF3, S (O) pCHF2, CN or halogen; a second R4 is H, F, Cl, Br, I or CF3 ; R6 is Cl-C4 alkyl, Cl-C4 haloalkyl, halogen or CN R6 is CH3, CF3 or halogen; R7 is CH3, CF3 or halogen; and p is 0, 1 or 2.

Preferred 15. Methods of Preferred 14 wherein

R3 is Cl-C4 alkyl ; one R4 group is attached to the K-ring at the 2-position and said R4 is CH3, Cl or Br ; a second R4 is H, F, Cl, Br, I or CF3 ; R6 is Cl or Br; and R7 is halogen or CF3.

Preferred 16. Methods of Preferred 9 wherein J substituted with 1 to 3 Rs is J-9 ; R3 is Cl-C4 alkyl optionally substituted with halogen, CN, OCH3, S (O) pCH3 ; one R4 group is attached to the K-ring at the 2-position and said R4 is CH3, CF3, OCF3, OCHF, S (O) pCF3, S (O) pCHF2, CN or halogen; a second R4 is H, F, Cl, Br, I or CF3; R6 is Cl-C4 alkyl, Cl-C4 haloalkyl, halogen or CN; R7 is CH3, CF3 or halogen; and pis0, 1 or2.

Preferred 17. Methods of Preferred 18 wherein R3 is Cl-C4 alkyl ; one R4 group is attached to the K-ring at the 2-position and said R4 is CH3, Cl or Br; a second R4 is H, F, Cl, Br, I or CF3 ; R6 is Cl or Br; and R7 is CF3.

Preferred 18. Methods of Preferred 9 wherein J substituted with 1 to 3 R5 is J-10 ; R3 is Cl-C4 alkyl optionally substituted with halogen, CN, OCH3, S (O) pCH3; one R4 group is attached to the K-ring at the 2-position and said R4 is CH3, CF3, OCF3, OCHF2, S (O) pCF3, S (O) pCHF2, CN or halogen; a second R4 is H, F, Cl, Br, I or CF3 ; R6 is Cl-C4 alkyl, Cl-C4 haloalkyl, halogen or CN; R9 is C2-C6 alkyl or Cl-C6 haloalkyl ; and p is 0, 1 or 2.

Preferred 19. Methods of Preferred 1 S wherein R3 is Cl-C4 alkyl ; one R4 group is attached to the K-ring at the 2-position and said R4 is CH3, Cl or Br ; a second R4 is H, F, Cl, Br, I or CF3; R6 is Cl or Br; and R9 is CF3, CHF2, CBrF7, CClF2, CH2CF3, or CF2CHF2.

Preferred 20. Methods of Preferred 9 wherein J substituted with 1 to 3 R5 is J-11 ; R3 is Cl-C4 alkyl optionally substituted with halogen, CN, OCH3, S (O) pCH3; one R4 group is attached to the K-ring at the 2-position and said R4 is CH3, CF3, OCF3, OCHF2, S (O) pCF3, S (O) pCHF2, CN or halogen; a second R4 is H, F, Cl, Br, I or CF3; R6 is Cl-C4 alkyl, Cl-C4 haloalkyl, halogen or CN; R7 is CH3, CF3, OCHF2 or halogen; and p is 0, 1 or 2.

Preferred 21. Methods of Preferred 20 wherein R3 is C1-C4 alkyl ; one R4 group is attached to the R-ring at the 2-position and said R4 is CH3, Cl or Br ; a second R4 is H, F, Cl, Br, I or CF3; R6 is Cl or Br; and R7 is halogen or CF3.

Preferred 22. Methods of Preferred 9 wherein J substituted with 1 to 3 R5 is J-12; R3 is Cl-C4 alkyl optionally substituted with halogen, CN, OCH3, S (O) pCH3; one R4 group is attached to the K-ring at the 2-position and said R4 is CH3, CF3, OCF3, OCHF2, S (O)pCF3, S (O) pCHF2, CN or halogen; a second R4 is H, F, Cl, Br, I or CF3; R6 is Cl-C4 alkyl, Cl-C4 haloalkyl, halogen or CN; R9 is C2-C6 alkyl or Cl-C6 haloalkyl ; and pis0, lor2.

Preferred 23. Methods of Preferred 22 wherein R3 is Cl-C4 alkyl ; one R4 group is attached to the K-ring at the 2-position and said R4 is CH3, Cl or Br ; a second R4 is H, F, Cl, Br, I or CF3; R6 is Cl or Br; and R9 is CF3, CHF2, CBrF2, CClF2, CHOC3, or CF2CHF2.

Preferred 24. Methods of Preferred 9 wherein J substituted with 1 to 3 R5 is J-13; R3 is Cl-C4 alkyl optionally substituted with halogen, CN, OCH3, S (O) pCH3 ; one R4 group is attached to the K-ring at the 2-position and said R4 is CH3, CF3, OCF3, OCHF2, S (O) pCF3, S (O) pCHF2, CN or halogen; a second R4 is H, F, Cl, Br, I or CF3;

R6 is Cl-C4 alkyl, Cl-C4 haloalkyl, halogen or CN; R9 is C2-C6 alkyl or C1-C6 haloalkyl ; and p is 0, 1 or 2.

Preferred 25. Methods of Preferred 24 wherein R3 is Cl-C4 alkyl ; one R4 group is attached to the K-ring at the 2-position and said R4 is CH3, Cl or Br ; a second R4 is H, F, Cl, Br, I or CF3 ; R6 is Cl or Br; and R9 is CF3, CHF, CBrF, CCIF, CH2CF3, or CF2CHF2.

Most preferred is the method wherein the compound of Formula I is selected from the group consisting of : 8-methyl-3- (l-methylethyl)-2- [2-methyl-6- (trifluoromethyl)-3-pyridinyl]-4 (3H)- quinazolinone, 2- [3-bromo-I- (3-chloro-2-pyridinyl)-lH-pyrazol-5-yl]-6-chloro-3, 8-dimethyl- 4(3H)-quinazoline, 2- [3-bromo-1- (3-chloro-2-pyridinyl)-lH-pyrazol-5-yl]-6-chloro-3-ethyl-S-m ethyl- 4(3H)-quinazoline, <BR> <BR> 2- [3-bromo-1- (3-chloro-2-pyridinyl)-lH-pyrazol-5-yl]-6-chloro-8-methyl-3- <BR> <BR> <BR> (1-methylethyl)-4 (31)-quinazoline,<BR> <BR> <BR> 2- [3-bromo-1- (3-chloro-2-pyridinyl)-1H-pyrazol-5-yl]-6-chloro-3- (1,1-dimethylethyl)-8-methyl-4 (3H)-quinazoline, 6-chloro-2- [3-chloro-1- (3-chloro-2-pyridinyl)-lH-pyrazol-5-yl]-3, 8-dimethyl- 4(3H)-quinazoline, 6-chloro-2- [3-chloro-1- (3-chloro-2-pyridinyl)-1H-pyrazol-5-yl]-3-ethyl-8-methyl- 4 (3H)-quinazoline, 6-chloro-2-[3-chloro-1-(3-chloro-2-pyridinyl)-1H-pyrazol-5-y l]-8-methyl-3- (1-methylethyl)-4 (3H)-quinazoline, 6-chloro-2-[3-chloro-1-(3-chloro-2-pyridinyl)-1H-pyrazol-5-y l]-3- (1, 1-dimethylethyl)-8-methyl-4(3H)-quinazoline, 6-chloro-2-[1-(3-chloro-2-pyridinyl)-3-(trifluoromethyl)-1H- pyrazol-5-yl]-3,8- dimethyl-4 (3H)-quinazoline, 6-chloro-2-[1-(3-chloro-2-pyridinyl)-3-(trifluoromethyl)-1H- pyrazol-5-yl]-3-ethyl- 8-methyl-4 (3H)-quinazoline, 6-chloro-2-[1-(3-chloro-2-pyridinyl)-3-(trifluoromethyl)-1H- pyrazol-5-yl]-8- methyl-3-(1-methylethyl)-4(3H)-quinazoline, 6-chloro-2-[1-(3-chloro-2-pyridinyl)-3-(trifluoromethyl)-1H- pyrazol-5-yl]-3- (1, 1-dimethylethyl)-8-methyl-4 (3H)-quinazoline,

2- [3-bromo-1- (3-chloro-2-pyridinyl)-1H-pyrazol-5-yl]-8-methyl-3- (l-methylethyl)- 4 (3H)-quinazoline, 2- [3-bromo-1- (3-chloro-2-pyridinyl)-lH-pyrazol-5-yl]-3- (l, 1-dimethylethyl)-8- methyl-4 (3H)-quinazoline, <BR> <BR> <BR> 2- [1- (3-chloro-2-pyridinyl)-3- (trifluoromethyl)-1H-pyrazol-5-yl]-8-methyl-3-<BR> <BR> <BR> <BR> <BR> <BR> (1-methylethyl)-4 (3H)-quinazoline,<BR> <BR> <BR> <BR> <BR> <BR> 2- [l- (3-chloro-2-pyridinyl)-3- (trifluoromethyl)-1H-pyrazol-5-yl]-3- (1,1-dimethylethyl)-8-methyl-4 (3H)-quinazoline, 6,8-dichloro-2- [1- (3-chloro-2-pyridinyl)-3- (trifluoromethyl)-1H-pyrazol-5-yl]-3- methyl-4 (3H)-quinazoline, 6,8-dichloro-2- [l- (3-chloro-2-pyridinyl)-3- (trifluoromethyl)-1H-pyrazol-5-yl]-3- ethyl-4 (3H)-quinazoline, 6,8-dichloro-2- [l- (3-chloro-2-pyridinyl)-3- (trifluoromethyl)-1H-pyrazol-5-yl]-3- (l- methylethyl)-4 (3H)-quinazoline, 2-[3-bromo-1-(3-chloro-2-pyridinyl)-1H-pyrazol-5-yl]-6,8-dic hloro-3-methyl- 4 (3H)-quinazoline, 2-[3-bromo-1-(3-chloro-2-pyridinyl)-1H-pyrazol-5-yl]-6,8-dic hloro-3-ethyl-4(3H0- quinazoline, 2- [3-bromo-1- (3-chloro-2-pyridinyl)-1H-pyrazol-5-yl]-6, 8-dichloro-3- (1-methylethyl)-4 (3H)-quinazoline, 6,8-dichloro-2- [3-chloro-1- (3-chloro-2-pyridinyl)-1H-pyrazol-5-yl]-3-methyl- 4 (3H)-quinazoline, 6,8-dichloro-2- [3-chloro-1- (3-chloro-2-pyridinyl)-1H-pyrazol-5-yl]-3-ethyl-4 (3H)- quinazoline, and 6, 8-dichloro-2-[3-chloro-1-(3-chloro-2-pyridinyl)-1H-pyrazol-5 -yl]-3- (1-methylethyl)-4 (3H)-quinazoline.

Preferred compounds for reasons of better activity, cost and/or ease of synthesis are: Preferred A. Compounds of Formula la wherein J substituted with 1 to 3 R5 is J-6; R3 is C1-C4 alkyl optionally substituted with halogen, CN, OCH3, S (O) pCH3; one R4 group is attached to the K-ring at the 2-position and said R4 is CH3, CF3, OCF3, OCHF2, S (O) pCF3, S (O) pCHF, CN or halogen ; a second R4 is H, F, Cl, Br, I or CF3; R6 is Cl-C4 alkyl, Cl-C4 haloalkyl, halogen or CN; R7 is CH3, CF3, OCHF2 or halogen; and pis0, 1 or 2.

Preferred B. Compounds of Preferred A wherein R3 is Cl-C4 alkyl ;

one R4 group is attached to the IL-ring at the 2-position and said R4 is CH3, Cl or Br ; a second R4 is H, F, Cl, Br, I or CF3; R6 is Cl or Br; and R7 is halogen or CF3.

Preferred C. Compounds of Formula la wherein J substituted with 1 to 3 R5 is J-7; R3 is Cl-C4 alkyl optionally substituted with halogen, CN, OCH3, S (O) pCH3; one R4 group is attached to the K-ring at the 2-position and said R4 is CH3, CF3, OCF3, OCHF2, S (O) pCF3, S (O) pCHF2, CN or halogen; a second R4 is H, F, Cl, Br, I or CF3 ; R6 is C1-C4 alkyl, C1-C4 haloalkyl, halogen or CN; R9 is C2-C6 alkyl or C1-C6 haloalkyl ; and p is 0, 1 or 2.

Preferred D. Compounds of Preferred C wherein R3 is C1-C4 alkyl ; one R4 group is attached to the K-ring at the 2-position and said R4 is CH3, Cl or Br ; a second R4 is H, F, Cl, Br, I or CF3; R6 is Cl or Br; and R9 is CF3, CHF2, CBrF2, CClF2, CH2CF3, or CF2CHF2.

Preferred E. Compounds of Formula la wherein J substituted with 1 to 3 R5 is J-8 ; R3 is Cl-C4 alkyl optionally substituted with halogen, CN, OCH3, S (O) pCH3; one R4 group is attached to the K-ring at the 2-position and said R4 is CH3, CF3, OCF3, OCHFo, S (O) pCF3, S (O) pCHF, CN or halogen; a second R4 is H, F, Cl, Br, I or CF3; R6 is C1-C4 alkyl, C1-C4 haloalkyl, halogen or CN R6 is CH3, CF3 or halogen; R7 is CH3, CF3 or halogen; and p is 0, 1 or 2.

Preferred F. Methods of Preferred E wherein R3 is C1-C4 alkyl ; one R4 group is attached to the K-ring at the 2-position and said R4 is CH3, Cl or Br ; a second R4 is H, F, Cl, Br, I or CF3; R6 is Cl or Br; and R7 is halogen or CF3.

Preferred G. Compounds of Formula Ia wherein J substituted with 1 to 3 R5 is J-9 ; R3 is C1-C4 alkyl optionally substituted with halogen, CN, OCH3, S (O) pCH3; one R4 group is attached to the K-ring at the 2-position and said R4 is CH3, CF3, OCF3, OCHF, S (O) pCF3, S (O) pCHF2, CN or halogen; a second R4 is H, F, Cl, Br, I or CF3 ; R6 is C1-C4 alkyl, C1-C4 haloalkyl, halogen or CN; R7 is CH3, CF3 or halogen; and p is 0, 1 or 2.

Preferred H. Compounds of Preferred G wherein R3 is C 1-C4 alkyl ; one R4 group is attached to the K-ring at the 2-position and said R4 is CH3, Cl or Br ; a second R4 is H, F, Cl, Br, I or CF3; R6 is Cl or Br; and R7 is CF3.

Preferred I. Compounds of Formula la wherein J substituted with 1 to 3 R5 is J-10; R3 is C1-C4 alkyl optionally substituted with halogen, CN, OCH3, S (O) pCH3; one R4 group is attached to the K-ring at the 2-position and said R4 is CH3, CF3, OCF3, OCHF2, S (O) pCF3, S (O) pCHF2, CN or halogen; a second R4 is H, F, Cl, Br, I or CF3; R6 is C1-C4 alkyl, C1-C4 haloalkyl, halogen or CN; R9 is C2-C6 alkyl or C1-C6 haloalkyl ; and p is 0, 1 or 2.

Preferred J. Compounds of Preferred I wherein R3 is C1-C4 alkyl ; one R4 group is attached to the K-ring at the 2-position and said R4 is CH3, Cl or Br ; a second R4 is H, F, Cl, Br, I or CF3; R6 is Cl or Br; and R9 is CF3, CHF2, CBrF2, CClF2, CH2CF3, or CF2CHF2.

Preferred K. Compounds of Formula Ia wherein J substituted with 1 to 3 R5 is J-11 ; R3 is C1-C4 alkyl optionally substituted with halogen, CN, OCH3, S (O) pCH3 ; one R4 group is attached to the K-ring at the 2-position and said R4 is CH3, CF3, OCF3, OCHF2, S (O) pCF3, S (O) pCHF2, CN or halogen; a second R4 is H, F, CI, Br, I or CF3;

R6 is C1-C4 alkyl, C1-C4 haloalkyl, halogen or CN; R7 is CH3, CF3, OCHF2 or halogen; and p is 0, 1 or 2.

Preferred L. Compounds of Preferred K wherein R3 is Cl-C4 alkyl ; one R4 group is attached to the K-ring at the 2-position and said R4 is CH3, Cl or Br ; a second R4 is H, F, Cl, Br, I or CF3; R6 is Cl or Br; and R7 is halogen or CF3.

Preferred M. Compounds of Formula Ia wherein J substituted with 1 to 3 R5 is J-12; R3 is C1-C4 alkyl optionally substituted with halogen, CN, OCH3, S (O) pCH3 ; one R4 group is attached to the K-ring at the 2-position and said R4 is CH3, CF3, OCF3, OCHF2, S (O) pCF3, S (O) pCHF2, CN or halogen; a second R4 is H, F, Cl, Br, I or CF3; R6 is C1-C4 alkyl, C1-C4 haloalkyl, halogen or CN; R9 is C2-C6 alkyl or C1-C6 haloalkyl ; and p is 0, 1 or 2.

Preferred N. Methods of Preferred M wherein R3 is C1-C4 alkyl ; one R4 group is attached to the K-ring at the 2-position and said R4 is CH3, Cl or Br ; a second R4 is H, F, Cl, Br, I or CF3 ; R6 is Cl or Br; and R9 is CF3, CHF2, CBrF, CClF2, CH2CF3, or CF2CHF2.

Preferred O. Compounds of Formula Ia wherein J substituted with 1 to 3 R5 is J-13; R3 is C1-C4 alkyl optionally substituted with halogen, CN, OCH3, S (O) pCH3; one R4 group is attached to the K-ring at the 2-position and said R4 is CH3, CF3, OCF3, OCHF2, S (O) pCF3, S (O) pCHF2, CN or halogen; a second R4 is H, F, Cl, Br, I or CF3; R6 is C1-C4 alkyl, C1-C4 haloalkyl, halogen or CN; R9 is C2-C6 alkyl or C1-C6 haloalkyl ; and p is 0, 1 or 2.

Preferred P. Methods of Preferred O wherein R3 is C1-C4 alkyl ;

one R4 group is attached to the K-ring at the 2-position and said R4 is CH3, Cl or Br ; a second R4 is H, F, Cl, Br, I or CF3 ; R6 is Cl or Br; and R9 is CF3, CHF2, CBrF2, CC1F2, CH2CF3, or CF2CHF2.

Most preferred is the compound of Formula I selected from the group consisting of: 8-methyl-3- (l-methylethyl)-2- [2-methyl-6- (trifluoromethyl)-3-pyridinyl]-4 (3H)- quinazolinone, 2- [3-bromo-1- (3-chloro-2-pyridinyl)-1H-pyrazol-5-yl]-6-chloro-3, 8-dimethyl- 4 (3H)-quinazoline, 2- [3-bromo-1- (3-chloro-2-pyridinyl)-lH-pyrazol-5-yl]-6-chloro-3-ethyl-8-m ethyl- 4(3H)-quinazoline, 2- [3-bromo-1- (3-chloro-2-pyridinyl)-1H-pyrazol-5-yl]-6-chloro-8-methyl-3- (1-methylethyl)-4(3H)-quinazoline, 2- [3-bromo-1- (3-chloro-2-pyridinyl)-1H-pyrazol-5-yl]-6-chloro-3- (1,1-dimethylethyl)-8-methyl-4(3H)-quinazoline, 6-chloro-2- [3-chloro-1- (3-chloro-2-pyridinyl)-1H-pyrazol-5-yl]-3, 8-dimethyl- 4 (3H)-quinazoline, 6-chloro-2- [3-chloro-1- (3-chloro-2-pyridinyl)-1H-pyrazol-5-yl]-3-ethyl-8-methyl- 4(3H)-quinazoline, 6-chloro-2- [3-chloro-1- (3-chloro-2-pyridinyl)-1H-pyrazol-5-yl]-8-methyl-3- (1-methylethyl)-4 (3H)-quinazoline, 6-chloro-2- [3-chloro-1- (3-chloro-2-pyridinyl)-1H-pyrazol-5-yl]-3- (1,1-dimethylethyl)-8-methyl-4(3H)-quinazoline, 6-chloro-2- [1- (3-chloro-2-pyridinyl)-3- (trifluoromethyl)-1H-pyrazol-5-yl]-3, 8- dimethyl-4(3H)-quinazoline, 6-chloro-2- [l- (3-chloro-2-pyridinyl)-3- (trifluoromethyl)-1H-pyrazol-5-yl]-3-ethyl- 8-methyl-4 (3H)-quinazoline, 6-chloro-2-[1-(3-chloro-2-pyridinyl)-3-(trifluoromethyl)-1H- pyrazol-5-yl]-8- methyl-3- (1-methylethyl)-4 (3H)-quinazoline, 6-chloro-2-[1-(3-chloro-2-pyridinyl)-3-(trifluoromethyl)-1H- pyrazol-5-yl]-3- (1, 1-dimethylethyl)-8-methyl-4 (3H)-quinazoline, 2- [3-bromo-1- (3-chloro-2-pyridinyl)-1H-pyrazol-5-yl]-8-methyl-3- (l-methylethyl)- 4(3H)-quinazoline, 2-[3-bromo-1-(3-chloro-2-pyridinyl)-1H-pyrazol-5-yl]-3-(1,1- dimethylethyl)-8- methyl-4(3H)-quinazoline, 2-[1-(3-chloro-2-pyridinyl)-3-(trifluoromethyl)-1H-pyrazol-5 -yl]-8-methyl-3- (1-methylethyl)-4(3H)-quinazoline,

2- [1- (3-chloro-2-pyridinyl)-3- (trifluoromethyl)-lH-pyrazol-5-yl]-3- (1,1-dimethylethyl)-8-methyl-4 (3H)-quinazoline, 6,8-dichloro-2- [l- (3-chloro-2-pyridinyl)-3- (trifluoromethyl)-1H-pyrazol-5-yl]-3- methyl-4 (3H)-quinazoline, 6,8-dichloro-2- [l- (3-chloro-2-pyridinyl)-3- (trifluoromethyl)-1H-pyrazol-5-yl]-3- ethyl-4(3H)-quinazoline, 6,8-dichloro-2-[1-(3-chloro-2-pyridinyl)-3-(trifluoromethyl) -1H-pyrazol-5-yl]-3-(1- methylethyl)-4 (3H)-quinazoline, 2- [3-bromo-1- (3-chloro-2-pyridinyl)-1H-pyrazol-5-yl]-6, 8-dichloro-3-methyl- 4(3H)-quinazoline, 2- [3-bromo- 1- (3-chloro-2-pyridinyl)-IH-pyrazol-5-yl]-6, 8-dichloro-3-ethyl-4 (3H)- quinazoline, 2- [3-bromo-1- (3-chloro-2-pyridinyl)-1H-pyrazol-5-yl]-6, 8-dichloro-3- (1-methylethyl)-4 (3H)-quinazoline, 6,8-dichloro-2- [3-chloro-1- (3-chloro-2-pyridinyl)-lH-pyrazol-5-yl]-3-methyl- 4 (3H)-quinazoline, 6,8-dichloro-2- [3-chloro-1- (3-chloro-2-pyridinyl)-lH-pyrazol-5-yl]-3-ethyl-4 (3H)- quinazoline, and 6,8-dichloro-2- [3-chloro-1- (3-chloro-2-pyridinyl)-1H-pyrazol-5-yl]-3- (1-methylethyl)-4 (3H)-quinazoline.

This invention also pertains to a composition for controlling an invertebrate pest comprising a biologically effective amount of a compound of Formula la and at least one additional component selected from the group consisting of surfactants, solid diluents and liquid diluents. Preferred compositions are those comprising the above preferred compounds.

Of note is a method for controlling arthropods comprising contacting the arthropods or their environment with an arthropodicidally effective amount of a compound of Formula 1, its N-oxides or agriculturally suitable salts thereof wherein BisOorS ;

J is a phenyl group substituted with 1 to 2 R5 and optionally substituted with 1 to 3 R6, or a 5-or 6-membered heteroaromatic ring optionally substituted with 1 to 4 R7 ; n is 1 to 4 ; R3 is C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C3-C6 cycloalkyl, each optionally substituted with one or more substituents selected from the group consisting of halogen, CN, NO2, hydroxy, Cl-C4 alkoxy, C1-C4 alkylthio, C1-C4 alkylsulfinyl and Cl-C4 alkylsulfonyl ; C1-C4 alkoxy; C1-C4 alkylamino ; C2-C8 dialkylamino; C3-C6 cycloalkylamino; C2-C6 alkoxycarbonyl or C2-C6 alkylcarbonyl; each R4 is independently H, C1-Cg alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C3-C6 cycloalkyl, C1-C6 haloalkyl, C2-C6 haloalkenyl, C2-C6 haloalkynyl, C3-C6 halocycloalkyl, halogen, CN, CO2H, CONH2, N02, hydroxy, C1-C4 alkoxy, C1-C4 haloalkoxy, C1-C4 alkylthio, C1-C4 alkylsulfinyl, C1-C4 alkylsulfonyl, C1-C4 haloalkylthio, C1-C4 haloalkylsulfinyl, C1-C4 haloalkylsulfonyl, C1-C4 alkylamino, C2-C8 dialkylamino, C3-C6 cycloalkylamino, C2-C6 alkylcarbonyl, C2-C6 alkoxycarbonyl, C2-C6 alkylaminocarbonyl, C3-C8 dialkylaminocarbonyl, C3-C6 trialkylsilyl; or each R4 is independently phenyl, benzyl or phenoxy, each optionally substituted with Cl-C4 alkyl, Co-C4 alkenyl, C2-C4 alkynyl, C3-C6 cycloalkyl, C1-C4 haloalkyl, C2-C4 haloalkenyl, C2-C4 haloalkynyl, C3-C6 halocycloalkyl, halogen, CN, NO2, C1-C4 alkoxy, C1-C4 haloalkoxy, C1-C4 alkylthio, C1-C4 alkylsulfinyl, Cl-C4 alkylsulfonyl, C1-C4 alkylamino, C2-Cg dialkylamino, C3-Cg cycloalkylamino, C3-C6 (alkyl) cycloalkylamino, C2-C4 alkylcarbonyl, C2-C6 alkoxycarbonyl, C2-Cg alkylaminocarbonyl, C3-C8 dialkylaminocarbonyl or C3-C6 trialkylsilyl; each R5 is independently C1-C6 alkyl, C2-C6 alkenyl, C2-Cg alkynyl, C3-C6 cycloalkyl, C1-C6 haloalkyl, Cl--C6 haloalkenyl, C2-C6 haloalkynyl, C3-C6 halocycloalkyl, halogen, CN, CO2H, CONH2, N02, hydroxy, C1-C4 alkoxy, C1-C4 haloalkoxy, C1-C4 alkylthio, C1-C4 alkylsulfinyl, C1-C4 alkylsulfonyl, C1-C4 haloalkylthio, C1-C4 haloalkylsulfinyl, C1-C4 haloalkylsulfonyl, C1-C4 alkylamino, C2-Cg dialkylamino, C3-C6 cycloalkylamino, C2-C6 alkylcarbonyl, C ?--C6 alkoxycarbonyl, C2-C6 alkylaminocarbonyl, Cg-Cg dialkylaminocarbonyl, C3-C6 trialkylsilyl; or (R5) 2 when attached to adjacent carbon atoms can be taken together as -OCF2O-, -CF2CF2O-, or -OCF2CF2O-; each R6 is independently H, halogen, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C3-C6 cycloalkyl, CI-C4 alkoxy or C2-C4 alkoxy carbonyl; or each R6 is independently a phenyl, benzyl, phenoxy or a 5-or 6-membered heteroaromatic ring, each ring optionally substituted with C1-C4 alkyl, C2-C4

alkenyl, C2-C4 alkynyl, C3-C6 cycloalkyl, C1-C4 haloalkyl, C2-C4 haloalkenyl, C2-C4 haloalkynyl, C3-C6 halocycloalkyl, halogen, CN, NO2, C1-C4 alkoxy, C1-C4 haloalkoxy, C1-C4 alkylthio, C1-C4 alkylsulfinyl, C1-C4 alkylsulfonyl, C1-C4 alkylamino, C2-C8 dialkylamino, C3-C6 cycloalkylamino, C3-C6 (alkyl)cycloalkylamino, C2-C4 alkylcarbonyl, C2-C6 alkoxycarbonyl, C2-C6 alkylaminocarbonyl, C3-C8 dialkylaminocarbonyl or C3-C6 trialkylsilyl; each R7 is independently H, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C3-C6 cycloalkyl, C1-C6 haloalkyl, C2-C6 haloalkenyl, Cr-C6 haloalkynyl, C3-C6 halocycloalkyl, halogen, CN, C02H, CONH2, NO2, hydroxy, Cl-C4 alkoxy, C1-C4 haloalkoxy, C1-C4 alkylthio, Cl-C4 alkylsulfinyl, Cl-C4 alkylsulfonyl, C1-C4 haloalkylthio, C1-C4 haloalkylsulfinyl, Cl-C4 haloalkylsulfonyl, Ci-C4 alkoxycarbonyl, Ci-C4 alkylamino, C2-Cg dialkylamino, C3-C6 cycloalkylamino, C2-C6 alkylcarbonyl, C2-C6 alkoxycarbonyl, C2-C6 alkylaminocarbonyl, C3-Cg dialkylaminocarbonyl, C3-C6 trialkylsilyl ; or each R7 is independently a phenyl, benzyl, benzoyl, phenoxy or a 5-or 6-membered heteroaromatic ring, each ring optionally substituted with C1-C4 alkyl, C2-C4 alkenyl, C2-C4 alkynyl, C3-C6 cycloalkyl, C1-C4 haloalkyl, C2-C4 haloalkenyl, C2-C4 haloalkynyl, C3-C6 halocycloalkyl, halogen, CN, NO2, C1-C4 alkoxy, C1-C4 haloalkoxy, C1-C4 alkylthio, C1-C4 alkylsulfinyl, C1-C4 alkylsulfonyl, C1-C4 alkylamino, C2-C8 dialkylamino, C3-C6 cycloalkylamino, C3-C6 (alkyl) cycloalkylamino, C2-C4 alkylcarbonyl, C' ?-C6 alkoxycarbonyl, C2-C6 alkylaminocarbonyl, C3-Cg dialkylaminocarbonyl or C3-C6 trialkylsilyl.

Of note are compounds of Formula 1 wherein 1 B is O ; J is a phenyl group substituted with 1 to 2 R5 and optionally substituted with 1 to 3 R6 ; or J is selected from the group consisting of pyridine, pyrimidine, pyrazole, thiophene and thiazole, each optionally substituted with 1 to 3 R7 ; R3 is C2-C4 alkyl optionally substituted with halogen, CN, OCH3, S (O) pCH3; each R4 is independently CH3, CF3, OCF3, OCHF2, S (O) pCF3, S (O) pCHF2 or halogen;

each R5 is independently CF3, OCF3, OCHF2, S (O) pCF3, S (O) pCHF2, OCH2CF3, OCF2CHF2, S (O) pCH,) CF3 or S (O) pCF2CHF2 ; each R6 is independently halogen or methyl; or phenyl, pyrazole, imidazole, triazole, pyridine or pyrimidine, each ring optionally substituted with C1-C4 alkyl, C1-C4 haloalkyl, halogen or CN; each R7 is independently H, halogen, CH3, CF3, OCHF2, S (O) pCF3, S (O) pCHF2, OCH2CF3, OCF2CHF2, S (O) pCH2CF3, S (O) pCF2CHF2 ; or phenyl, pyrazole, imidazole, triazole, pyridine or pyrimidine, each ring optionally substituted with C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, C1-C4 haloalkoxy, halogen, NO-) or CN; and p is 0, 1 or 2.

As noted above, J is a phenyl ring, a naphthyl ring system, a 5-or 6-membered heteroaromatic ring or an aromatic 8-, 9-or 10-membered fused heterobicyclic ring system wherein each ring or ring system is optionally substituted with 1 to 4 R5. The tenn "optionally substituted"in connection with these J groups refers to groups which are unsubstituted or have at least one non-hydrogen substituent that does not extinguish the biological activity possessed by the unsubstituted analog. An example of phenyl optionally substituted with 1 to 4 R5 is the ring illustrated as U-1 in Exhibit 1, wherein Rv is R5 and r is an integer from 1 to 4. An example of a naphthyl group optionally substituted with 1 to 3 R5 is illustrated as U-85 in Exhibit 1, wherein Rv is R5 and r is an integer from 1 to 4.

Examples of 5-or 6-membered heteroaromatic rings optionally substituted with 1 to 4 R5 include the rings U-2 through U-53 illustrated in Exhibit 1 wherein Rv is R5 and r is an integer from 1 to 4. Note that J-1 through J-5 below also denote 5-or 6-membered heteroaromatic rings. Note that U-2 through U-20 are examples of J-1, U-21 through U-35 and U-40 are examples of J-2, U-36 through U-39 are examples of J-3, U-41 through U-48 are examples of J-4 and U-49 through U-53 are examples of J-5. Examples of aromatic 8-, 9-or 10-membered fused heterobicyclic ring systems optionally substituted with 1 to 4 R5 include U-54 through U-84 illustrated in Exhibit 1 wherein Rv is R5 and r is an integer from 1 to 4.

Although Rv groups are shown in the structures U-1 through U-85, it is noted that they do not need to be present since they are optional substituents. Note that when Rv is H when attached to an atom, this is the same as if said atom is unsubstituted. The nitrogen atoms that require substitution to fill their valence are substituted with H or Rv. Note that some U groups can only be substituted with less than 4 Rv groups (e. g. U-14, U-15, U-18 through U-21 and U-32 through U-34 can only be substituted with one RV). Note that when the attachment point between (RV) r and the U group is illustrated as floating, (RV) r can be attached to any available carbon atom of the U group. Note that when the attachment point on the U group is illustrated as floating, the U group can be attached to the remainder of Formula I through any available carbon of the U group by replacement of a hydrogen atom.

Exhibit 1

As noted above G can be a 5-or 6-membered nonaromatic carbocyclic or heterocyclic ring, optionally including one or two ring members selected from the group consisting of C (=O), SO or S (O) and optionally substituted with 1 to 4 substituents selected from Rl". Examples of such G groups include those illustrated as G-1 through G-41 in Exhibit 2 wherein m is an integer from 1 to 4. The term"optionally substituted"in connection with these G groups refers to groups which are unsubstituted or have at least one non-hydrogen substituent that does not extinguish the biological activity possessed by the unsubstituted analog. Although (Rl2) m are illustrated in the examples, they need not be present since they are optional substituents. Note that when the attachment point on these G groups is illustrated as floating, the G group can be attached to the remainder of Formula I through any available carbon or nitrogen of the G group by replacement of a hydrogen atom.

The optional substituents can be attached to any available carbon or nitrogen by replacing a hydrogen atom. Note that when G comprises a ring selected from G-24 through G-29 and G-32 through G-35, A is selected from O, S, NH or NR12. Note that when G is G-3, G-5, G-7, G-9, G-16 through G-18, G-23, and G-24 through G-29, and G-32 through G-35 (when A is NR12), the nitrogen atoms that require substitution to fill their valence are substituted with H or R12.

Exhibit 2

G-37 G-38 G-39 G-40 G-41 As noted above, R3 can be (among others) C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C3-C6 cycloalkyl, each optionally substituted with one or more substituents selected from (among others) a phenyl, phenoxy or 5-or 6-membered heteroaromatic ring, each ring optionally substituted with one to three substituents independently selected from R6. The term"optionally substituted"in connection with these groups refers to groups which are unsubstituted or have at least one non-hydrogen substituent that does not extinguish the biological activity possessed by the unsubstituted analog. Examples of such substituents include the rings illustrated as U-1 through U-53 and U-88 illustrated in Exhibit 1, except that such rings are optionally substituted with 1 to 3 substituents independently selected from R6 rather than (RV) r. Note that R6 substituents do not need to be present since they are optional substituents.

As noted above, each R4 is independently (among others) a phenyl, benzyl, phenoxy or a 5-or 6-membered heteroaromatic ring, each ring optionally substituted with one to three substituents independently selected from R6. The term"optionally substituted"in connection with these R4 groups refers to groups which are unsubstituted or have at least one non-hydrogen substituent that does not extinguish the biological activity possessed by the unsubstituted analog. Examples of such R4 groups include the rings illustrated as U-1 through U-53, U-86 and U-88 illustrated in Exhibit 1, except that such rings are optionally substituted with 1 to 3 substituents independently selected from R6 rather than (RV) r. Note that R6 substituents do not need to be present since they are optional substituents.

As noted above, each R5 is independently (among others) a phenyl, benzyl, benzoyl, phenoxy, 5-or 6-membered heteroaromatic ring or an aromatic 8-, 9-or 10-membered fused heterobicyclic ring system, each ring optionally substituted with one to three substituents independently selected from R6. Examples of such R5 groups include the rings illustrated as U-1 through U-88 illustrated in Exhibit 1, except that such rings are optionally substituted with 1 to 3 substituents independently selected from R6 rather than (RV) r. Note that R6 substituents do not need to be present since they are optional substituents. Note that in J-6 through J-13, R7 and R9 are subsets of R5.

As noted above K is, together with the two contiguous linking carbon atoms, a fused phenyl or a fused pyridinyl ring optionally substituted with 1 to 4 R4. The term"optionally substituted"in connection with these K groups refers to groups which are unsubstituted or have at least one non-hydrogen substituent that does not extinguish the biological activity

possessed by the unsubstituted analog. Examples of such K groups include the rings illustrated as K-1 through K-5 in Exhibit 3. Note that K-2 through K-5 can be optionally substituted with one to three 3 R4 groups. In the exemplified K groups, the upper right bond is attached through the available linking carbon atom to the nitrogen atom of the N=C-J portion of Formula I and the lower right bond is attached through the available linking carbon atom to the carbon atom of the C (=B) NR3 portion of Formula I. The wavy line indicates that the K-ring is attached to the remainder of Formula I as illustrated below.

Exhibit 3 Preferred K-rings are K-1, K-2 and K-5. Most preferred is K-1.

The compounds of Formula I can be prepared by one or more of the following methods and variations as described in Schemes 1-13. The definitions of B, J, K, R3, R4, R5 and n in the compounds of Formulae I and 2-24 below are as defined above in the Summary of the Invention. Of note are compounds wherein K is K-1.

Compounds of Formula Ib (Formula I wherein B is O) can be prepared by procedures outlined in Schemes 1-13. A typical procedure is detailed in Scheme 1 and involves dehydration of an o-amido amide of Formula 2 with sodium hydride and ethyl chloro formate in a suitable solvent (See e. g. Example 1). Other methods for preparing compounds of Formula I include treating a compound of Formula 2 with acetic anhydride and sodium acetate, heating at greater than 70 °C neat or optionally in an appropriate solvent such as tetrahydrofuran, and treating 2 with a suitable acid scavenger and trimethylsilyl chloride in a

suitable solvent. Further useful methods include heating o-amido amides of Formula 2 adsorbed on surface-active materials such as zeolites or clay, generally in the range of 50-150 °C. A specific example of this type is described in Example 2 and involves heating the anthranilic amide on Montmorillonite clay. Compounds of Formula Ic (Formula I wherein B is S) can be prepared by conventional methods for conversion of amides to thioamides such as by treatment with phosphorus pentasulfide or Lawesson's reagent. (See (Bull. Soc. Chim. Belg.), 1978,87,229; and (Tett-clzednofr Lett.), 1983,24,3S15 for general procedures).

Scheme 1 Oq/J 4) n 4 H Dehydration O H R3 \, Tj p3 2 Ib (B is O) Ic (B is S) Compounds of Formula 2 can be prepared by procedures outlined in Scheme 2. A typical procedure involves coupling of an o-amino amide of Formula 3 with an acid chloride of Formula 4 in the presence of an acid scavenger to provide the compound of Formula 2.

Typical acid scavengers include amine bases such as triethylamine, diisopropylethylamine and pyridine; other scavengers include hydroxides such as sodium and potassium hydroxide and carbonates such as sodium carbonate and potassium carbonate. In certain instances it is useful to use polymer-supported acid scavengers such as polymer-bound diisopropylethylamine and polymer-bound dimethylaminopyridine.

Scheme 2

3 4 2 An alternate procedure for the preparation of compounds of Formula 2 involves coupling of an o-amino amide of Formula 3 with an acid of Formula 5 in the presence of a

dehydrating agent such as dicyclohexylcarbodiimide (DCC). Polymer supported reagents can be useful here, such as polymer-bound cyclohexylcarbodiimide. Synthetic procedures of Schemes 2 and 3 are only representative examples of useful methods for the preparation of Formula 2 compounds as the synthetic literature is extensive for this type of reaction.

Scheme 3 O>J lq, n dehydrative coupling reagent OH OH ont 3

5 2 One skilled in the art will also realize that acid chlorides of Formula 4 may be prepared from acids of Formula 5 by numerous well-known methods.

Formula 3 o-Amino amides are typically available from the corresponding o-nitro amides of Formula 6 via catalytic hydrogenation of the nitro group. Typical procedures involve reduction with hydrogen in the presence of a metal catalyst such as palladium on carbon or platinum oxide and in hydroxylic solvents such as ethanol and isopropanol. These procedures are well documented in the chemical literature.

Scheme 4 NO (R4) n reduction a° a0 /\ 3 Hz \ R3

6 3 The intermediate amides of Formula 6 are readily prepared from commercially available o-nitro acids of Formula 7. Typical methods for amide formation can be applied here. These include direct dehydrative coupling of acids of Formula 7 with amines of Formula 8 using for example DCC, and conversion of the acids to an activated form such as the acid chlorides or anhydrides and subsequent coupling with amines to form amides of Formula 6. Ethylchloroformate is an especially useful reagent for this type of reaction.

Scheme 5 k (D 4 ) Amide formation K N O OH/\ 3 7 8 6

Intermediate o-amino amides of Formula 3 may also be prepared from anhydrides of Formula 9 (Scheme 6). Typical procedures involve combination of equimolar amounts of the amine 8 with the anhydride of Formula 9 in polar aprotic solvents such as pyridine and dimethylformamide at temperatures ranging from room temperature to 100 °C.

Scheme 6

An alternate procedure for the preparation of compounds of Formula 2 involves reaction of an amine 8 with a compound of Formula 10. Typical procedures involve combination of the amine with the compound of Formula 10 in solvents such as tetrahydrofuran or pyridine at temperatures ranging from room temperature to the reflux temperature of the solvent. Benzoxazinones (compounds of Formula 10 wherein K is K-1) are well documented in the chemical literature and are available via known methods that involve the coupling of either an anthranilic acid or an isatoic anhydride with an acid chloride.

Scheme 7

10 8 2 Compounds of Formula I may also be prepared by modification of known procedures (J. Med. Claim. 1985,28,568). Usually this involves condensation of an aryl aldehyde of Formula 11 with a compound of Formula 3 in an alcoholic solvent and with a catalytic amount of base to produce intermediate 12, which is then further oxidized to the Formula I compound by known methods. This reaction is shown in Scheme 8.

Scheme 8 H (R4) n NH, (R4) n I i oxidation K! + J-CHO JL if!) + J-CHO base / alcohol N R 11 H/N\R3 ° 12 3 An alternate procedure for the preparation of specific quinazolinones of Formula I (Formula Id) is depicted in Scheme 9. This procedure may be specifically suitable for pyrazole-substituted quinazolinones which may prove difficult to prepare by alternate procedures. The cross coupling reaction of quinazolines of Formula 13 (wherein X is a leaving group such as halogen, triflate or fluorosulfonate) with pyrazoles of Formula 14 (where Met is Sn, Zn, B (OH) 2, Mg, Li or Cu and additional counterions as necessary) in the presence of a palladium or nickel catalyst produces compounds of Formula Id. Quinazolines of Formula 13 wherein X is halogen are known in the art (PCT patent application publication W098/26664 and references cited therein). Preferred catalysts for the synthesis of compounds of Formula Id include but are not limited to Pd (PPh3) 4, PdClo (PPh3), PdCl2(diphenylphosphinoferrocene), NiCl2(PPh3)2, and Tetrakis (tri-2- furylphosphino) palladium. The exact conditions for each reaction depend upon the catalyst used and the metal attached to the pyrazole. The additional presence of an external base (such as an alkali carbonate, tertiary amine or alkali fluoride) is necessary for reactions involving pyrazoles of Formula 14 where Met is B (OH) 2. Similar procedures also can be used for other K-rings and J-groups.

Scheme 9 0/ O N/Pd or Ni R4) ; + Met) ~ R6 > R6 catalyst + Met x N (R4) n N 13 14 n RS 13 14 0 X is halogen or sulfonate Met is Sn, Zn, B (OH) 2, Mg, Li or Cu < R6 is Cl, Br or CF3 6 pin N N (R4) n 14N M j N Id R5

Pyrazoles of Formula 14 can be made by lithiation of the pyrazole 17 followed by transmetallation with the appropriate metal as described in Scheme 10. Pyridylpyrazoles 17 are prepared by the reaction of pyrazoles 15 with a 2,3-dihalopyridine of Formula 16 to afford the 1-pyridylpyrazole 17 with good specificity for the desired regiochemistry.

Metallation of 17 with lithium diisopropylamide (LDA) followed by transmetallation with the appropriate metal affords the metal pyrazole of Formula 14. For conditions and catalysts used in transmetallation and cross coupling reactions see Metal-catalyzed Cross-coupling Redactions. Diederich, Francois; Stang, Peter J.; Editors. 1998, p. 517, (Wiley-VCH, Weinheim, Germany) and references cited therein.

Scheme 10

14 The starting pyrazoles 15 are known compounds. Pyrazole 15 wherein R5 is CF3 is commercially available. Pyrazoles 15 wherein R5 is Cl or Br can be prepared by literature procedures (Chem. Ber. 1966,99 (10), 3350-7). A useful alternative method for the preparation of 15 wherein R5 is Cl or Br is depicted in Scheme 11. Metallation of the sulfamoyl pyrazole 19 with 71-butyllithium followed by direct halogenation of the anion with either hexachloroethane (for R5 being Cl) or 1,2-dibromotetrachloroethane (for R5 being Br) affords the halogenated derivatives 20. Removal of the sulfamoyl group with tlifluoroacetic acid (TFA) at room temperature proceeds cleanly and in good yield to afford the pyrazoles 15 wherein R5 is Cl or Br respectively. One skilled in the art will recognize that Formula 15c is a tautomer of Formula 15b.

Scheme 11

An alternate procedure for the preparation of quinazolinones of Formula Id involves prolonged heating of a benzoxazinone of Formula 21 with an amine of Formula 22 as shown in Scheme 12. Reactions times as long as 1-7 days may be required. An example of this type is detailed in Example 3. Similar procedures also can be used for other K-rings and J-groups.

Scheme 12

The benzoxazinones of Formula 21 are available by the method of Scheme 13.

Coupling of a pyrazole acid of Formula 23 with an anthranilic acid of Formula 24 via sequential addition of methanesulfonyl chloride and triethylamine affords the benzoxazinone of Formula 21. The intermediate acid of Formula 23 is available from the lithiated pyrazole 18 by quenching with carbon dioxide. Similar procedures also can be used for other K-rings and J-groups.

Scheme 13

It is recognized that some reagents and reaction conditions described above for preparing compounds of Formula I may not be compatible with certain functionalities present in the intermediates. In these instances, the incorporation of protection/deprotection

sequences or functional group interconversions into the synthesis will aid in obtaining the desired products. The use and choice of the protecting groups will be apparent to one skilled in chemical synthesis (see, for example, Greene, T. W.; Wuts, P. G. M. Protective Groups i7z Oi-ga7liC SvjrtlTesis, 2nd ed.; Wiley: New York, 1991). One skilled in the art will recognize that, in some cases, after the introduction of a given reagent as it is depicted in any individual scheme, it may be necessary to perform additional routine synthetic steps not described in detail to complete the synthesis of compounds of Formula I. One skilled in the art will also recognize that it may be necessary to perform a combination of the steps illustrated in the above schemes in an order other than that implied by the particular sequence presented to prepare the compounds of Formula I.

One skilled in the art will also recognize that compounds of Formula I and the intermediates described herein can be subjected to various electrophilic, nucleophilic, radical, organometallic, oxidation, and reduction reactions to add substituents or modify existing substituents.

Without further elaboration, it is believed that one skilled in the art using the preceding description can utilize the present invention to its fullest extent. The following Examples are, therefore, to be construed as merely illustrative, and not limiting of the disclosure in any way whatsoever. Percentages are by weight except for chromatographic solvent mixtures or where otherwise indicated. Parts and percentages for chromatographic solvent mixtures are by volume unless otherwise indicated. 1H NMR spectra are reported in ppm downfield from tetramethylsilane; s is singlet, d is doublet, t is triplet, q is quartet, m is multiplet, dd is doublet of doublets, dt is doublet of triplets, br s is broad singlet.

EXAMPLE 1 Preparation of 8-methyl-3-(1-methylethyl)-2-[2-methyl-4-(trifluoromethyl)ph enyl]-4(3H)- quinazolinone Step A: Preparation of 3-methyl-N-(1-methrlethyl)-2-nitrobenzamide A solution of 3-methyl-2-nitrobenzoic acid (2.00 g, 11.0 mmol) and triethylamine (1.22 g, 12. 1 mmol) in 25 mL of methylene chloride was cooled to 10°C. Ethyl chloroformate was carefully added and a solid precipitate formed. After stirring for 30 minutes isopropylamine (0.94 g, 16. 0 mmol) was added and a homogeneous solution resulted. The reaction was stirred for an additional hour, poured into water and extracted with ethyl acetate. The organic extracts were washed with water, dried over magnesium sulfate and evaporated under reduced pressure to afford 1.96 g of the desired intermediate as a white solid melting at 126-128 °C.

1H NMR (CDC13) 8 1.24 (d, 6H), 2.38 (s, 3H), 4.22 (m, lH), 5.80 (br s, lH), 7.4 (m, 3H).

Step B: Preparation of 2-amino-3-methyl1-methylethyl) benzamide The 2-nitrobenzamide of Step A (1.70 g, 7.6 mmol) was hydrogenated over 5% Pd/C in 40 mL of ethanol at 3.45 X 105 Pa. When the uptake of hydrogen ceased the reaction was filtered through celite and the celite was washed with ether. The filtrate was evaporated under reduced pressure to afford 1.41 g of the title compound as a solid melting at 149-151 °C.

IH NMR (CDC13) 6 1.24 (dd, 6H), 2.16 (s, 3H), 4.25 (m, lH), 5.54 (br s, 2H), 5.85 (br s, lH), 6.59 (t, lH), 7.13 (d, lH), 7.17 (d, lH).

Step C: Preparation of S, S-dimethyl-N-[4-(triluoromethyl)phenyl]sulfilimine A solution ofN-chlorosuccinimide (12.43 g, 93.1 mmol) in-170 mL of dichloromethane was added to a mixture of 4- (trifluoromethyl) aniline (15 g, 93.1 mmol) and dimethyl sulphide (6.35 g, 102 mmol) in 230 mL of dichloromethane at-5 to 0 °C.

After the addition was complete, the mixture was stirred at 0-5 °C for 1 hour, and N-chlorosuccinimide (0.02 g, 4.64 mmol) was added. After a further 30 minutes, the mixture was washed with 500 mL of IN sodium hydroxide.

The organic phase was dried and evaporated to give the product as a solid 19.72 g melting at 101-103 °C (after crystallization from ethyl acetate/hexanes).

IR (lfujolt)) 1603, 1562,1532, 1502, 1428,1402,1335,1300,1270,1185,1150, 1103,1067,1000,972,940,906,837,817 cm-1.

IH NMR (CDC13) 8 7.35 (d, 2H), 6.84 (d, 2H), 2. 67 (s, 3H).

Step D: 2- [ methyl]-4-(trifluoromethYl) benzenamine Sodium methoxide in methanol (1.95 g, 9.02 mmol, 25%) was added to S, S-dimethyl-N [4- (trifluoromethyl) phenyl] sulfilimine from Step C (2 g, 9.04 mmol) in 15 mL of toluene. The mixture was warmed to-80°C for-1 h. The mixture was allowed to cool to 25 °C and was poured into 100 mL of water. The mixture was extracted with 2x100 mL of ethyl acetate and the combined extracts were dried and evaporated to give the product 1.8 g as a solid melting at 65.5-67.5 °C (after crystallization from hexanes).

IR (Nujolg) 3419,3333,1629,1584,1512,1440,1334,1302,1235,1193,1139, 1098,1078,979,904,832 cm.

IH NMR (CDC13) 6 7.35 (dd, lH), 7.26 (s, lH), 6. 72 (d, lH) 4.39 (br s, 2H), 3.69 (s, 2H), 1.99 (s, 3H).

Step E: Preparation of 2-methyl-4-(trifluoromethyl) benzenamine Activated Raney nickel (500 g wet paste, #50µ) was added portionwise to a solution of 2- [(methylthio) methyl]-4-(trifluoromethyl) benzenamine (55.3 g, 0.25 mole) in 1 L of ethanol over 30 minutes at 25-30 °C. The heterogeneous mixture was stirred vigorously for 30 minutes after the addition. The stirring was stopped, and the solids were allowed to settle over one hour. The liquid was decanted from the solids and poured through filter paper.

The filtrate was evaporated under reduced pressure, and the residue was taken up in

dichloromethane. The organic phase was separated from a small volume of water, dried over magnesium sulfate and evaporated under reduced pressure to afford 37.6 g of the title compound as an amber oil.

IH NMR (CDCI3) 6 7.28 (m, 2H), 6.68 (d, lH), 3.87 (br s, 2H), 2.19 (s, 3H).

Step F: Preparation of 2-methyl-4- (trifluoromethyl) benzonitrile Concentrated hydrochloric acid (16 mL) was added dropwise at a moderate rate to a heterogeneous mixture of 2-methyl-4- (trifluoromethyl) benzenamine (14 g, 80 mmol) and 120 mL of water while stirring vigorously. A thick suspension resulted which was stirred for 20 minutes, diluted with 280 mL of water and cooled to 5 °C. A solution of sodium nitrite (5.5 g, SO mmol) in 25 mL of water was added slowly to the reaction suspension. After stirring for 30 minutes at 5 °C a solution resulted which was stirred cold for 30 more minutes and then neutralized with potassium carbonate. This diazonium salt solution was then added portionwise via cannula to a stirred, 95 °C mixture of potassium cyanide (22 g, 0.34 mole), copper sulfate pentahydrate (20 g, 80 mmol) and 140 mL of water. After the addition the mixture was stirred for 30 minutes at 95 °C and then allowed to cool to room temperature.

Ether was added and the heterogeneous mixture was filtered through celite. The solids were washed with ether, and the filtrate was partitioned. The aqueous phase was extracted with ether, and the combined organic extracts were dried over magnesium sulfate and concentrated under reduced pressure to afford 13.1 g of the title compound as a brown oil.

IH NMR (CDCI3) 8 7.74 (d, lH), 7.60 (s, lH), 7.55 (d, lH), 2.64 (s, 3H).

Step G: Preparation of 2-methyl-4-trifluoromethyl benzoic acid Potassium hydroxide (15.7 g, 0.28 mole) and 15 mL of water were added as a solution to a stirred, heterogeneous mixture of 2-methyl-4- (trifluoromethyl) benzonitrile (13 g, 70 mmol) and 135 mL of ethylene glycol. The reaction mixture was heated at 120-130 °C for 20 hours and allowed to cool to room temperature. The dark solution was poured into 800 mL of water and filtered through celite. The filtrate was washed with ether and then the aqueous was acidified with concentrated hydrochloric acid. This aqueous phase was extracted three times with ethyl acetate, the organic extracts were combined, dried over magnesium sulfate and evaporated under reduced pressure to afford the title compound as a tan solid.

I H NMR (CDC13) S 7.98 (d, lH), 7.70 (s, lH), 7.65 (d, lH), 2.60 (s, 3H).

Step H : Preparation of 9-methyl-4-(trifluoromethoxy ! benzovl chloride Thionyl chloride (0.42 g, 3.5 mmol) was added to a solution of the benzoic acid from Step G (0.50 g, 2.4 mmol) in 10 mL of toluene at room temperature. The reaction was refluxed for three hours then cooled to room temperature. The solvent was evaporated under reduced pressure and excess thionyl chloride was removed by azeotroping with toluene. The benzoyl chloride obtained was used directly in Step I.

Step I : Preparation of 2-methyl-N-[2-methyl-6-[[(1-methylethyl)amino]- carbonyl] phenyl]-4- (trifluoromethyl) benzamide The benzoyl chloride of Step H (0.29 g, 1.3 mmol) was added to a mixture of the aniline from Step B (0.36 g, 1.9 mmol) and diisopropylethylamine (0.26 g, 2.0 mmol) in 10 mL of chloroform at room temperature. The reaction was allowed to stir overnight. The solid precipitate was filtered and dried to afford 0.38 g of the title compound, as a solid melting at 247-248 °C.

IH NMR (CDC13) 5 1. 24 (d, 6H), 2.41 (s, 3H), 2. 58 (s, 3H), 4.20 (m, lH), 5.94 (br d, lH), 7.2-7.3 (m, 2H), 7.40 (d, lH), 7.52 (s, lH), 7.53 (d, lH), 7.70 (d, lH), 9.36 (br s, lH).

Step J: Preparation of 8-methyl-3-(1-methylethyl)-2-[2-methyl-4- (trifluoromethyl) phenyl]-4 (3H)-quinazolinone A slurry of the benzamid of Step I (0.25 g, 0.6 mmol) in N, N-dimethylformamide (4 mL) was added cautiously to a slurry of NaH (0.03 g, 0.7 mmol, 60%) in N, N-dimethylformamide (2 mL). Gas evolution was seen and the mixture became a light yellow solution. After stirring for approximately 5 min, methylchloroformate (0.11 g, 1.2 mmol) was added and a solid precipitate formed. The reaction was stirred for 30 min, then poured into water (50 mL) and extracted with ethyl acetate (2x50 mL). The combined extracts were washed with water (2x50 mL) then dried and evaporated to give 0.16 g of the title compound, a compound of the invention, as a solid melting at 100-103 °C.

IH NMR (CDC13) 8 1.25 (d, 6H), 2.52 (s, 3H), 2.81 (s, 3H), 4. 28 (m, lH), 7.26 (t, lH), 7.43 (d, lH), 7.57-7.61 (br s, 2H), 7.98 (d, lH), 8. 07 (d, lH).

EXAMPLE 2 Preparation of 6-chloro-2- [1- (3-chloro-2-pyridinyl)-3- (trifluoromethyl)-1H-pyrazol-5-yll- 3, 8-dimethyl-4 (377)-quinazoline Step A: Preparation of 2-amino-3-methvl-5-chlorobenzoic acid To a solution of 2-amino-3-methylbenzoic acid (Aldrich, 15.0 g, 99.2 mmol) in N, N-dimethylformamide (50 mL) was added N-chlorosuccinimide (13.3 g, 99.2 mmol) and the reaction mixture was heated to 100 °C for 30 minutes. The heat was removed, the reaction was cooled to room temperature and let stand overnight. The reaction mixture was then slowly poured into ice-water (250 mL) to precipitate a white solid. The solid was filtered and washed four times with water and then taken up in ethyl acetate (900 mL). The ethyl acetate solution was dried over magnesium sulfate, evaporated under reduced pressure and the residual solid was washed with ether to afford the desired intermediate as a white solid (13.9 g).

IH NMR (DMSO-d6) 8 2.11 (s, 3H), 7.22 (s, 1H), 7.55 (s, 1H).

Step B: Preparation of 3-chloro-2- [3- (trifluoromethyl-lH-pvrazol-1-yl] pyridine To a mixture of 2, 3-dichloropyridine (99.0 g, 0.67 mol) and 3-trifluoromethyl pyrazole (83 g, 0.61 mol) in dry N, N-dimethylformamide (300 mL) was added potassium carbonate (166.0 g, 1.2 mot) and the reaction was then heated to 110-125 °C over 48 hours. The reaction was cooled to 100 °C and filtered through CeliteW diatomaceous filter aid to remove solids. N, N-Dimethylformamide and excess dichloropyridine were removed by distillation at atmospheric pressure. Distillation of the product at reduced pressure (b. p. 139-141 °C, 7 mm) afforded the desired intermediate as a clear yellow oil (113.4 g).

1H NMR (CDC13) 8 6.78 (s, 1H), 7.36 (t, 1H), 7.93 (d, 1H), 8.15 (s, 1H), 8.45 (d, 1H).

Step C: Preparation of 1- !-3-(trifluoromethYl)-lH-pYrazole-5- carboxylic acid To a solution of the pyrazole product from Step B (105.0 g, 425 mmol) in dry tetrahydrofuran (700 mL) at-75 °C was added via cannula a-30 °C solution of lithium diisopropylamide (425 mmol) in dry tetrahydrofuran (300 mL). The deep red solution was stirred for 15 minutes, after which time carbon dioxide was bubbled through at-63 °C until the solution became pale yellow and the exothernaicity ceased. The reaction was stirred for an additional 20 minutes and then quenched with water (20 mL). The solvent was removed under reduced pressure, and the reaction mixture partitioned between ether and 0.5 N aqueous sodium hydroxide solution. The aqueous extracts were washed with ether (3x), filtered through Celite# diatomaceous filter aid to remove residual solids, and then acidified to a pH of approximately 4, at which point an orange oil formed. The aqueous mixture was stirred vigorously and additional acid was added to lower the pH to 2. 5-3. The orange oil congealed into a granular solid, which was filtered, washed successively with water and IN hydrochloric acid, and dried under vacuum at 50 °C to afford the title product as an off-white solid (130 g). (Product from another run following similar procedure melted at 175-176 °C.) 1H NMR (DMSO-d6) 8 7.61 (s, 1H), 7.76 (dd, 1H), 8.31 (d, 1H), S. 60 (d, 1H).

Step D: Preparation of 6-chloro-2-[1-(3-chloro-2-pyridinyl)-3-(trifluoromethyl)-1H- pYrazol-5-yl]-8-methyl-4H-3 1-benzoxazin-4-one To a solution of methanesulfonyl chloride (2.2 mL, 28. 3 mmol) in acetonitrile (75 mL) was added dropwise a mixture of the carboxylic acid product from Step C (7. 5 g, 27.0 mmol) and triethylamine (3.75 mL, 27.0 mmol) in acetonitrile (75 mL) at 0-5 °C. The reaction temperature was then maintained at 0 °C throughout successive addition of reagents. After stirring for 20 minutes, 2-amino-3-methyl-5-chlorobenzoic acid from Step A (5.1 g, 27.0 mmol) was added and stirring was continued for an additional 5 minutes. A solution of triethylamine (7.5 mL, 54.0 mmol) in acetonitrile (15 mL) was then added dropwise, and the reaction mixture was stirred 45 minutes, followed by the addition of methanesulfonyl chloride (2. 2 mL, 28.3 mmol). The reaction mixture was then warmed to room temperature and stirred overnight. Approximately 75 mL of water was then added to precipitate 5.8 g of

a yellow solid. An additional 1 g of product was isolated by extraction from the filtrate to provide a total of 6.8 g of the title compound as a yellow solid.

1H NMR (CDC13) 8 1.83 (s, 3H), 7.50 (s, 1H), 7.53 (m, 2H), 7.99 (m, 2H), 8. 58 (d, 1H).

Step E: Preparation of N-[4-chloro-2-methyl-6-[(methylamino)carbonyl]phenyl]-1-(3- chloro-2-pyridinyl)-3-!-lH-pyrazole-5-carboxamide To a solution of the benzoxazinone product of Step D (6.6 g, 15 mmol) in tetrahydrofuran (50 mL) was added methylamine (2.0 M solution in THF, 38 mL, 77.38 mmol), and the reaction mixture was heated to 60 °C, stirred for 1 hour and then cooled to room temperature. The tetrahydrofuran solvent was evaporated under reduced pressure, and the residual solid was purified by chromatography on silica gel to afford the title compound, as a white solid melting at 225-226 °C.

I H NMR (CDC13) # 2. 17 (s, 3H), 2.95 (m, 3H), 6.2 (m, 1H), 7.2 (m, 2H), 7.4 (m, 2H), 7.85 (md, lH), S. 45 (md, lH), 10.2 (br s, 1H).

Step F: Preparation of 6-chloro-2- [l- (3-chloro-2-pvridinyl)-3- (trifluoromethv)-1H- pyrazol-5-yl]-3,8-dimethyl-4 (I)-quinazoline A solution of the title compound from Step E (50 mg, 0.11 mmol) in dichloromethane (20 mL) was mixed with 2 g of montmorillonite K10 clay (Aldrich, preactivated by heating under vacuum) and evaporated to dryness iii vaczio. The dry residue was heated using a steam bath (ca. 90-95 °C) for a total of 24 hours. The solids were then extracted twice by mixing with dichloromethane and ethyl acetate (1: 1) and filtering. The combined filtrates were evaporated to leave a film. This material was chromatographed on silica gel using 5% ethyl acetate in dichloromethane as the eluant. Pure fractions were combined, evaporated and the residue crystallized from dichloromethane/hexanes to afford 15 mg of the title compound, a compound of the invention, as a white solid.

IR (KBr) 1674,1598,1462,1241,1194,1169,1140 cm-1.

1H NMR (CDC13) 6 2.10 (s, 3H), 3.78 (s, 3H), 7.06 (s, 1H), 7.37 (dd, lH), 7.42 (d, lH), 7.87 (dd,1 H).

EXAMPLE 3 Preparation of 8-chloro-2-[1-(3-chloro-2-pyridinyl)-3-(trifluoromethyl)-1H- pyrazol-5-yl]-3- methyl-4 (3H)-quinzolinone Step A: Preparation of 8-chloro-2-[1-(3-chloro-2-pyridinyl)-3-(trifluoromethyl)-1H- pyrazol-5-yll-4H-3, 1-benzoxazin-4-one Application of the procedure of Example 2, Step D with 2.91 g of the carboxylic acid of Example 2, Step C and 1.71 g of 2-amino-3-chlorobenzoic acid affords 2.5 g of the title benzoxazinone.

IH NMR (CDC13) 8 7.46 (t, lH), 7.50 (m, lH), 7.52 (s, lH), 7.76 (d, lH), 8. 00 (d, lH), 8.11 (d, lH), 8. 58 (d, lH).

Step B: Preparation of 8-chloro-2- [ (3-chloro-2-pvridinvl)-3- (trifluoromethvl)-lH- pyrazol-5-yl]-3-methyl-4 (3H-quinazolinone A solution of the title compound of Step A (300 mg) in 2 mL of tetrahydrofuran was treated with methylamine (2.0 M solution in THF, 10 mL), sealed in a capped bottle and stirred for four days at room temperature. The solvent was removed under reduced pressure and the solid residue was washed with ether. The ether soluble material was purified by chromatography on silica gel using hexanes/ethyl acetate (1 : 1) as eluant. The title compound, a compound of the invention, was isolated as a solid, m. p. 155-157 °C.

H NMR (CDC13) 8 3.8 (s, 3H), 7.1 (s, lH), 7.4 (m, 2H), 7.7 (d, lH), 7.9 (d, lH), 8. 15 (d, lH), 8.35 (m, lH).

By the procedures described herein together with methods known in the art, the following compounds of Tables 1 to 33 can be prepared. The following abbreviations are used in the Tables: t is tertiary, s is secondary, ra is normal, i is iso, c is cyclo, Me is methyl, Et is ethyl, Pr is propyl, i-Pr is isopropyl, t-Bu is tert butyl, Ph is phenyl, OMe is methoxy, OEt is ethoxy, SMe is methylthio, SEt is ethylthio, CN is cyano, NO2 is nitro, TMS is trimethylsilyl, S (O) Me is methylsulfinyl, and S (O) 2Me is methylsulfonyl.

Table 1 R5bisCl R5bisCF3 R5bisOCF3 R5bisCF (CF3) s R3 R4a R4b R3 R4a R4b R3 R4a R4b R3 R4a R4b i-Pr Me H i-Pr Me H i-Pr Me H i-Pr Me H i-Pr Cl H i-Pr CI H i-Pr Cl H i-Pr Cl H i-Pr Me Cl i-Pr Me Cl i-Pr Me Cl i-Pr Me Cl i-Pr Cl Cl i-Pr Cl Cl i-Pr Cl Cl i-Pr Cl Cl i-Pr Me Br i-Pr Me Br i-Pr Me Br i-Pr Me Br i-Pr Cl Br i-Pr Cl Br i-Pr Cl Br i-Pr Cl Br t-Bu Me H t-Bu Me H t-Bu Me H t-Bu Me H t-Bu CI H t-Bu Cl H t-Bu Cl H t-Bu Cl H t-Bu Me Cl t-Bu Me Cl t-Bu Me Cl t-Bu Me Cl t-Bu Cl Cl t-Bu Cl Cl t-Bu Cl Cl t-Bu Cl Cl t-Bu Me Br t-Bu Me Br t-Bu Me Br t-Bu Me Br R5b is Cl R5b is CF3 R5b is OCF3 R5b is CF(CF3)2 R3 R4a R4b R3 R4a R4b R3 R4a R4b R3 R4a R4b t-Bu Cl Br t-Bu Cl Br t-Bu Cl Br t-Bu Cl Br Et Me H Et Me H Et Me H Et Me H Et ci H Et ci H Et Cl H Et ci H Et Me Cl Et Me CI Et Me CI Et Me Cl Et ci ci Et Cl ci Et ci ci Et ci ci Et Me Br Et Me Br Et Me Br Et Me Br Et Cl Br Et Cl Br Et Cl Br Et Cl Br Me Me H Me Me H Me Me H Me Me H Me Cl H Me Cl H Me Cl H Me Cl H Me Me Cl Me Me CI Me Me Cl Me Me Cl Me Cl Cl Me Cl CI Me Cl Cl Me Cl Cl Me Me Br Me Me Br Me Me Br Me Me Br Me Cl Br Me Cl Br Me CI Br Me Cl Br Table 2 R5b is Cl R5b is CF3 R5b is OCF3 R5b is CF(CF3)2 R3 R4a R4b R3 R4a R4b R3 R4a R4b R3 R4a R4b i-Pr Me H i-Pr Me H i-Pr Me H i-Pr Me H i-Pr Cl H i-Pr Cl H i-Pr Cl H i-Pr Cl H i-Pr Me Cl i-Pr Me Cl i-Pr Me Cl i-Pr Me Cl i-Pr Cl Cl i-Pr Cl Cl i-Pr Cl Cl i-Pr Cl Cl i-Pr Me Br i-Pr Me Br i-Pr Me Br i-Pr Me Br i-Pr Cl Br i-Pr Cl Br i-Pr Cl Br i-Pr Cl Br t-Bu Me H t-Bu Me H t-Bu Me H t-Bu Me H t-Bu Cl H t-Bu Cl H t-Bu Cl H t-Bu Cl H t-Bu Me Cl t-Bu Me Cl t-Bu Me Cl t-Bu Me Cl t-Bu Cl Cl t-Bu Cl Cl t-Bu Cl Cl t-Bu Cl Cl t-Bu Me Br t-Bu Me Br t-Bu Me Br t-Bu Me Br t-Bu Cl Br t-Bu Cl Br t-Bu Cl Br t-Bu Cl Br R5b is Cl R5b is CF3 R5b is OCF3 R5b is CF(CF3)2 R3 R4a R4b R3 R4a R4b R3 R4a R4b R3 R4a R4b Et Me H Et Me H Et Me H Et Me H Et Cl H Et ci H Et Cl H Et ci H Et Me Cl Et Me Cl Et Me Cl Et Me Cl Et Cl Cl Et ci ci Et Cl Cl Et ci ci Et Me Br Et Me Br Et Me Br Et Me Br Et Cl Br Et Cl Br Et Cl Br Et Cl Br Me Me H Me Me H Me Me H Me Me H Me Cl H Me Cl H Me Cl H Me Cl H Me Me CI Me Me Cl Me Me Cl Me Me Cl Me Cl Cl Me Cl Cl Me CI Cl Me Cl Cl Me Me Br Me Me Br Me Me Br Me Me Br Me Cl Br Me Cl Br Me CI Br Me Cl Br Table 3 R5b is Cl R5b is CF3 R5b is OCF3 R5b is CF(CF3)2 R3 R4a R4b R3 R4a R4b R3 R4a R4b R3 R4a R4b i-Pr Me H i-Pr Me H i-Pr Me H i-Pr Me H i-Pr CI H i-Pr Cl H i-Pr Cl H i-Pr Cl H i-Pr Me Cl i-Pr Me Cl i-Pr Me Cl i-Pr Me Cl i-Pr Cl Cl i-Pr Cl Cl i-Pr Cl Cl i-Pr Cl Cl i-Pr Me Br i-Pr Me Br i-Pr Me Br i-Pr Me Br i-Pr Cl Br i-Pr Cl Br i-Pr Cl Br i-Pr Cl Br t-Bu Me H t-Bu Me H t-Bu Me H t-Bu Me H t-Bu Cl H t-Bu Cl H t-Bu Cl H t-Bu Cl H t-Bu Me Cl t-Bu Me Cl t-Bu Me Cl t-Bu Me Cl t-Bu Cl Cl t-Bu Cl Cl t-Bu Cl Cl t-Bu Cl Cl t-Bu Me Br t-Bu Me Br t-Bu Me Br t-Bu Me Br t-Bu Cl Br t-Bu Cl Br t-Bu Cl Br t-Bu Cl Br Et Me H Et Me H Et Me H Et Me H RSb is Cl R5b is CF3 R5b is OCF3 R5b is CF(CF3)2 R3 R4a R4b R3 R4a R4b R3 R4a R4b R3 R4a R4b Et ci H Et Ci H Et Ci H Et Cl H Et Me Cl Et Me Cl Et Me Cl Et Me Cl Et Cl Cl Et Cl Cl Et Cl Cl Et Cl Cl Et Me Br Et Me Br Et Me Br Et Me Br Et Cl Br Et Cl Br Et CI Br Et Cl Br Me Me H Me Me H Me Me H Me Me H Me Cl H Me Cl H Me Cl H Me Cl H Me Me Cl Me Me Cl Me Me Cl Me Me Cl Me Cl Cl Me Cl Cl Me Cl Cl Me Cl Cl Me Me Br Me Me Br Me Me Br Me Me Br Me Cl Br Me Cl Br Me Cl Br Me Cl Br Table 4 R5b is Cl R5b is CF3 R5b is OCF3 R5b is CF(CF3)2 R3 R4a R4b R3 R4a R4b R3 R4a R4b R3 R4a R4b i-Pr Me H i-Pr Me H i-Pr Me H i-Pr Me H i-Pr Cl H i-Pr Cl H i-Pr Cl H i-Pr Cl H i-Pr Me Cl i-Pr Me Cl i-Pr Me Cl i-Pr Me Cl i-Pr Cl Cl i-Pr Cl Cl i-Pr Cl Cl i-Pr Cl Cl i-Pr Me Br i-Pr Me Br i-Pr Me Br i-Pr Me Br i-Pr Cl Br i-Pr Cl Br i-Pr Cl Br i-Pr Cl Br t-Bu Me H t-Bu Me H t-Bu Me H t-Bu Me H t-Bu Cl H t-Bu Cl H t-Bu Cl H t-Bu Cl H t-Bu Me Cl t-Bu Me Cl t-Bu Me Cl t-Bu Me Cl t-Bu Cl Cl t-Bu Cl Cl t-Bu Cl Cl t-Bu Cl Cl t-Bu Me Br t-Bu Me Br t-Bu Me Br t-Bu Me Br t-Bu Cl Br t-Bu Cl Br t-Bu Cl Br t-Bu Cl Br Et Me H Et Me H Et Me H Et Me H Et Cl H Et Cl H Et Cl H Et Cl H R5b is Cl R5b is CF3 R5b is OCF3 R5b is CF(CF3)2 R3 R4a R4b R3 R4a R4b R3 R4a R4b R3 R4a R4b Et Me Cl Et Me Cl Et Me Cl Et Me Cl Et Cl Cl Et Cl ci Et Cl ci Et Cl ci Et Me Br Et Me Br Et Me Br Et Me Br Et Cl Br Et CI Br Et Cl Br Et Ci Br Me Me H Me Me H Me Me H Me Me H Me Cl H Me Cl H Me Cl H Me Cl H Me Me Cl Me Me Cl Me Me Cl Me Me Cl Me CI Cl Me Cl Cl Me Cl Cl Me Cl Cl Me Me Br Me Me Br Me Me Br Me Me Br Me Cl Br Me Cl Br Me Cl Br Me Cl Br Table 5 R3 R4a R4b RS R6 R3 R4a R4b RS R6 R3 R4a R4b R5 R6 Me CH3 H CF3 Cl Me CI H Cl Br Me Cl Br Cl Br Et CH3 H CF3 Cl Et Cl H Cl Br Et Cl Br Cl Br i-Pr CH3 H CF3 Cl i-Pr Cl H Cl Br i-Pr Cl Br Cl Br t-Bu CH3 H CF3 Cl t-Bu Cl H Cl Br t-Bu Cl Br Cl Br Me CH3 H CF3 Br Me Cl H Br Cl Me Cl Br Br Cl Et CH3 H CF3 Br Et Cl H Br Cl Et Cl Br Br Cl i-Pr CH3 H CF3 Br i-Pr Cl H Br Cl i-Pr Cl Br Br Cl t-Bu CH3 H CF3 Br t-Bu Cl H Br Cl t-Bu Cl Br Br Cl Me CH3 H Cl Cl Me Cl H Br Br Me Cl Br Br Br Et CH3 H CI Cl Et Cl H Br Br Et Cl Br Br Br i-Pr CH3 H Cl Cl i-Pr Cl H Br Br i-Pr Cl Br Br Br t-Bu CH3 H Cl Cl t-Bu Cl H Br Br t-Bu Cl Br Br Br Me CH3 H Cl Br Me Cl H CF3 Cl Me Cl I CF3 Cl Et CH3 H Cl Br Et Cl H CF3 Cl Et Cl I CF3 Cl i-Pr CH3 H Cl Br i-Pr Cl H CF3 Cl i-Pr Cl I CF3 Cl t-Bu CH3 H Cl Br t-Bu Cl H CF3 Cl t-Bu Cl I CF3 Cl R3 R4a R4b R5 R6 R3 R4a R4b R5 R6 R3 R4a R4b R5 R6 Me CH3 H Br Cl Me Cl H CF3 Br Me Cl I CF3 Br Et CH3 H Br Cl Et Cl H CF3 Br Et Cl I CF3 Br i-Pr CH3 H Br Cl i-Pr Cl H CF3 Br i-Pr Cl I CF3 Br t-Bu CH3 H Br Cl t-Bu Cl H CF3 Br t-Bu Cl I CF3 Br Me CH3 H Br Br Me Cl H Cl Cl Me Cl I Cl Cl Et CH3 H Br Br Et Cl H Cl CI Et Cl I Cl Cl i-Pr CH3 H Br Br i-Pr Cl H Cl Cl i-Pr Cl I Cl Cl t-Bu CH3 H Br Br i-Pr Cl H Cl Cl t-Bu Cl I Cl CI Me CH3 F CF3 Cl Me CH3 Cl CF3 Cl Me Cl I Cl Br Et CH3 F CF3 Cl Et CH3 Cl CF3 Cl Et CI I CI Br i-Pr CH3 F CF3 Cl i-Pr CH3 Cl CF3 Cl I-Pr Cl I Cl Br t-Bu CH3 F CF3 Cl t-Bu CH3 Cl CF3 Cl t-Bu Cl I Cl Br Me CH3 F CF3 Br Me CH3 Cl CF3 Br Me Cl I Br CI Et CH3 F CF3 Br Et CH3 Cl CF3 Br Et Cl I Br Cl i-Pr CH3 F CF3 Br i-Pr CH3 Cl CF3 Br i-Pr Cl I Br Cl t-Bu CH3 F CF3 Br t-Bu CH3 Cl CF3 Br t-Bu Cl I Br CI Me CH3 F Cl Cl Me CH3 Cl Cl Cl Me CI I Br Br Et CH3 F Cl Cl Et CH3 Cl Cl CI Et Cl I Br Br i-Pr CH3 F Cl Cl i-Pr cH3 Cl Cl Cl i-Pr Cl I Br Br t-Bu CH3 F Cl Cl t-Bu CH3 Cl Cl Cl t-Bu Cl I Br Br Me CH3 F Cl Br Me CH3 Cl Cl Br Me Cl CF3 CF3 Cl Et CH3 F Cl Br Et CH3 Cl Cl Br Et Cl CF3 CF3 Cl i-Pr CH3 F Cl Br i-Pr CH3 Cl Cl Br i-Pr Cl CF3 CF3 Cl t-Bu CH3 F Cl Br t-Bu CH3 Cl Cl Br t-Bu Cl CF3 CF3 Cl Me CH3 F Br Cl Me CH3 Cl Br Cl Me Cl CF3 CF3 Br Et CH3 F Br Cl Et CH3 Cl Br Cl Et Cl CF3 CF3 Br i-Pr CH3 F Br Cl i-Pr CH3 Cl Br Cl i-Pr Cl CF3 CF3 Br t-Bu CH3 F Br Cl t-Bu CH3 Cl Br Cl t-Bu Cl CF3 CF3 Br Me CH3 F Br Br Me CH3 Cl Br Br Me Cl CF3 Cl Cl Et CH3 F Br Br Et CH3 Cl Br Br Et Cl CF3 Cl Cl i-Pr CH3 F Br Br i-Pr CH3 Cl Br Br i-Pr Cl CF3 Cl Cl t-Bu CH3 F Br Br t-Bu CH3 Cl Br Br t-Bu Cl CF3 Cl Cl Me CH3 Br CF3 Cl Me Cl F CF3 Cl Me Cl CF3 Cl Br Et CH3 Br CF3 Cl Et Cl F CF3 Cl Et Cl CF3 Cl Br i-Pr CH3 Br CF3 Cl i-Pr Cl F CF3 Cl i-Pr Cl CF3 Cl Br t-Bu CH3 Br CF3 Cl t-Bu Cl F CF3 Cl t-Bu Cl CF3 Cl Br Me CH3 Br CF3 Br Me Cl F CF3 Br Me Cl CF3 Br CI R3 R4a R4b R5 R6 R3 R4a R4b R5 R6 R3 R4a R4b R5 R6 Et CH3 Br CF3 Br Et Cl F CF3 Br Et Cl CF3 Br Cl i-Pr CH3 Br CF3 Br i-Pr Cl F CF3 Br i-Pr Cl CF3 Br Cl t-Bu CH3 Br CF3 Br t-Bu Cl F CF3 Br t-Bu Cl CF3 Br Cl Me CH3 Br Cl Cl Me Cl F Cl Cl Me Cl CF3 Br Br Et CH3 Br Cl Cl Et Cl F Cl Cl Et Cl CF3 Br Br i-Pr CH3 Br Cl Cl i-Pr Cl F Cl Cl i-Pr Cl CF3 Br Br t-Bu CH3 Br Cl Cl t-Bu Cl F Cl Cl t-Bu Cl CF3 Br Br Me CH3 Br Cl Br Me Cl F Cl Br n-Pr Cl Cl Cl Cl Et CH3 Br Cl Br Et Cl F Cl Br n-Bu Cl Cl Cl Cl i-Pr CH3 Br Cl Br i-Pr Cl F Cl Br s-Bu Cl Cl Cl CI t-Bu CH3 Br Cl Br t-Bu Cl F Cl Br i-Bu Cl Cl Cl Cl Me CH3 Br Br Cl Me Cl F Br Cl Me Br F CF3 Cl Et CH3 Br Br Cl Et CI F Br Cl Et Br F CF3 Cl i-Pr CH3 Br Br Cl i-Pr Cl F Br Cl i-Pr Br F CF3 Cl t-Bu CH3 Br Br Cl t-Bu Cl F Br Cl t-Bu Br F CF3 Cl Me CH3 Br Br Br Me Cl F Br Br Me Br F CF3 Br Et CH3 Br Br Br Et Cl F Br Br Et Br F CF3 Br i-Pr CH3 Br Br Br i-Pr Cl F Br Br i-Pr Br F CF3 Br t-Bu CH3 Br Br Br t-Bu Cl F Br Br t-Bu Br F CF3 Br Me CH3 I CF3 Cl Me Cl Cl CF3 Cl Me Br F Cl Cl Et CH3 I CF3 Cl Et Cl Cl CF3 Cl Et Br F Cl Cl i-Pr CH3 I CF3 Cl i-Pr Cl Cl CF3 Cl i-Pr Br F Cl Cl t-Bu CH3 I CF3 Cl t-Bu Cl Cl CF3 Cl t-Bu Br F Cl Cl Me CH3 I CF3 Br Me Cl Cl CF3 Br Me Br F Cl Br Et CH3 I CF3 Br Et Cl Cl CF3 Br Et Br F Cl Br i-Pr CH3 I CF3 Br i-Pr Cl Cl CF3 Br i-Pr Br F Cl Br t-Bu CH3 I CF3 Br t-Bu Cl Cl CF3 Br t-Bu Br F Cl Br Me CH3 I Cl Cl Me Cl Cl Cl Cl Me Br F Br Cl Et CH3 I Cl Cl Et Cl Cl Cl Cl Et Br F Br ci i-Pr CH3 I Cl Cl i-Pr Cl Cl Cl Cl i-Pr Br F Br Cl t-Bu CH3 I Cl Cl t-Bu Cl Cl Cl Cl t-Bu Br F Br Cl Me CH3 I Cl Br Me Cl Cl Cl Br Me Br F Br Br Et CH3 I Cl Br Et Cl Cl Cl Br Et Br F Br Br i-Pr CH3 I Cl Br i-Pr Cl Cl Cl Br i-Pr Br F Br Br t-Bu CH3 I Cl Br t-Bu Cl Cl Cl Br t-Bu Br F Br Br Me CH3 I Br CI Me Br CF3 CF3 Cl Me Br Cl CF3 Cl Et CH3 I Br Cl Et Br CF3 CF3 Cl Et Br Cl CF3 Cl R3 R4a R4b R5 R6 R3 R4a R4b RS R6 R3 R4a R4b R5 R6 i-Pr CH3 I Br Cl i-Pr Br CF3 CF3 Cl i-Pr Br Cl CF3 Cl t-Bu CH3 I Br Cl t-Bu Br CF3 CF3 Cl t-Bu Br Cl CF3 Cl Me CH3 I Br Br Me Br CF3 CF3 Br Me Br Cl CF3 Br Et CH3 I Br Br Et Br CF3 CF3 Br Et Br Cl CF3 Br i-Pr CH3 I Br Br i-Pr Br CF3 CF3 Br i-Pr Br Cl CF3 Br t-Bu CH3 I Br Br t-Bu Br CF3 CF3 Br t-Bu Br Cl CF3 Br Me CH3 CF3 CF3 Cl Me Br CF3 Cl Cl Me Br Cl Cl Cl Et CH3 CF3 CF3 Cl Et Br CF3 Cl Cl Et Br Cl Cl Cl i-Pr CH3 CF3 CF3 Cl i-Pr Br CF3 Cl Cl i-Pr Br Cl Cl Cl t-Bu CH3 CF3 CF3 Cl t-Bu Br CF3 Cl Cl t-Bu Br Cl Cl Cl Me CH3 CF3 CF3 Br Me Br CF3 Cl Br Me Br Cl Cl Br Et CH3 CF3 CF3 Br Et Br CF3 Cl Br Et Br Cl Cl Br i-Pr CH3 CF3 CF3 Br i-Pr Br CF3 Cl Br i-Pr Br Cl Cl Br t-Bu CH3 CF3 CF3 Br t-Bu Br CF3 Cl Br t-Bu Br Cl Cl Br Me CH3 CF3 Cl Cl Me Br CF3 Br Cl Me Br Cl Br Cl Et CH3 CF3 Cl Cl Et Br CF3 Br Cl Et Br Cl Br Cl i-Pr CH3 CF3 Cl Cl i-Pr Br CF3 Br Cl i-Pr Br Cl Br Cl t-Bu CH3 CF3 Cl Cl t-Bu Br CF3 Br Cl t-Bu Br Cl Br CI Me CH3 CF3 Cl Br Me Br CF3 Br Br Me Br Cl Br Br Et CH3 CF3 Cl Br Et Br CF3 Br Br Et Br Cl Br Br i-Pr CH3 CF3 Cl Br i-Pr Br CF3 Br Br i-Pr Br Cl Br Br t-Bu CH3 CF3 Cl Br t-Bu Br CF3 Br Br t-Bu Br Cl Br Br Me CH3 CF3 Br Cl Me Br I CF3 Cl Me Br Br CF3 Cl Et CH3 CF3 Br Cl Et Br I CF3 Cl Et Br Br CF3 Cl i-Pr CH3 CF3 Br Cl i-Pr Br I CF3 Cl i-Pr Br Br CF3 Cl t-Bu CH3 CF3 Br Cl t-Bu Br I CF3 Cl t-Bu Br Br CF3 Cl Me CH3 CF3 Br Br Me Br I CF3 Br Me Br Br CF3 Br Et CH3 CF3 Br Br Et Br I CF3 Br Et Br Br CF3 Br i-Pr CH3 CF3 Br Br i-Pr Br I CF3 Br i-Pr Br Br CF3 Br t-Bu CH3 CF3 Br Br t-Bu Br I CF3 Br t-Bu Br Br CF3 Br n-pur CH3 Cl Cl Cl Me Br I Cl Cl Me Br Br Cl Cl -Bu CH3 Cl Cl Cl Et Br I Cl Cl Et Br Br Cl Cl s-Bu CH3 Cl Cl Cl i-Pr Br I Cl Cl i-Pr Br Br Cl Cl i-Bu CH3 Cl Cl Cl t-Bu Br I Cl Cl t-Bu Br Br Cl Cl Me Cl Cl Br Cl Me Br I Cl Br Me Br Br Cl Br Et Cl Cl Br Cl Et Br I Cl Br Et Br Br Cl Br i-Pr Cl Cl Br Cl i-Pr Br I Cl Br i-Pr Br Br Cl Br R3 R4a R4b R5 R6 R3 R4a R4b R5 R6 R3 R4a R4b R5 R6 t-Bu Cl Cl Br Cl t-Bu Br I Cl Br t-Bu Br Br Cl Br Me Cl Cl Br Br Me Br I Br Cl Me Br Br Br Cl Et Cl Cl Br Br Et Br I Br Cl Et Br Br Br Cl i-Pr Cl Cl Br Br i-Pr Br I Br Cl i-Pr Br Br Br Cl t-Bu Cl Cl Br Br t-Bu Br I Br CI t-Bu Br Br Br CI Me Cl Br CF3 Cl Me Br I Br Br Me Br Br Br Br Et Cl Br CF3 Cl Et Br I Br Br Et Br Br Br Br i-Pr Cl Br CF3 Cl i-Pr Br I Br Br i-Pr Br Br Br Br t-Bu Cl Br CF3 Cl t-Bu Br I Br Br t-Bu Br Br Br Br Me Cl Br CF3 Br Me Cl Br Cl Cl t-Bu Cl Br CF3 Br Et Cl Br CF3 Br Et Cl Br Cl Cl t-Bu Cl Br Cl Cl i-Pr Cl Br CF3 Br i-Pr Cl Br Cl Cl Table 6 R3 R4a R4b R5 R6 R3 R4a R4b R5 R6 R3 R4a R4b R5 R6 Me CH3 H CF3 Cl Me Cl H Cl Br Me Cl Br Cl Br Et CH3 H CF3 Cl Et Cl H Cl Br Et Cl Br Cl Br i-Pr CH3 H CF3 Cl i-Pr CI H Cl Br i-Pr Cl Br Cl Br t-Bu CH3 H CF3 Cl t-Bu Cl H Cl Br t-Bu Cl Br Cl Br Me CH3 H CF3 Br Me Cl H Br Cl Me Cl Br Br Ci Et CH3 H CF3 Br Et Cl H Br Cl Et Cl Br Br Cl i-Pr CH3 H CF3 Br i-Pr Cl H Br Cl i-Pr Cl Br Br Cl t-Bu CH3 H CF3 Br t-Bu Cl H Br Cl t-Bu Cl Br Br Cl Me CH3 H Cl Cl Me Cl H Br Br Me Cl Br Br Br Et CH3 H Cl Cl Et Cl H Br Br Et Cl Br Br Br i-Pr CH3 H Cl Cl i-Pr Cl H Br Br i-Pr Cl Br Br Br t-Bu CH3 H Cl Cl t-Bu Cl H Br Br t-Bu Cl Br Br Br Me CH3 H Cl Br Me Cl H CF3 Cl Me Cl I CF3 Cl Et CH3 H Cl Br Et Cl H CF3 Cl Et Cl I CF3 Cl i-Pr CH3 H Cl Br i-Pr Cl H CF3 Cl i-Pr Cl I CF3 Cl t-Bu CH3 H Cl Br t-Bu Cl H CF3 Cl t-Bu Cl I CF3 Cl R3 R4a R4b R5 R6 R3 R4a R4b R5 R6 R3 R4a R4b R5 R6 Me CH3 H Br Cl Me Cl H CF3 Br Me Cl I CF3 Br Et CH3 H Br Cl Et Cl H CF3 Br Et Cl I CF3 Br i-Pr CH3 H Br Cl i-Pr Cl H CF3 Br i-Pr Cl I CF3 Br t-Bu CH3 H Br Cl t-Bu Cl H CF3 Br t-Bu Cl I CF3 Br Me CH3 H Br Br Me Cl H Cl Cl Me Cl I Cl Cl Et CH3 H Br Br Et Cl H Cl Cl Et Cl I Cl Cl i-Pr CH3 H Br Br i-Pr Cl H Cl Cl i-Pr Cl I Cl Cl t-Bu CH3 H Br Br i-Pr Cl H Cl Cl t-Bu Cl I Cl Cl Me CH3 F CF3 Cl Me CH3 Cl CF3 Cl Me Cl I Cl Br Et CH3 F CF3 Cl Et CH3 Cl CF3 Cl Et Cl I Cl Br i-Pr CH3 F CF3 Cl i-Pr CH3 Cl CF3 Cl i-Pr Cl I Cl Br t-Bu CH3 F CF3 Cl t-Bu CH3 Cl CF3 Cl t-Bu Cl I Cl Br Me CH3 F CF3 Br Me CH3 Cl CF3 Br Me Cl I Br Cl Et CH3 F CF3 Br Et CH3 Cl CF3 Br Et Cl I Br Cl i-Pr CH3 F CF3 Br i-Pr CH3 Cl CF3 Br i-Pr Cl I Br Cl t-Bu CH3 F CF3 Br t-Bu CH3 Cl CF3 Br t-Bu Cl I Br Cl Me CH3 F Cl Cl Me CH3 Cl Cl Cl Me Cl I Br Br Et CH3 F Cl Cl Et CH3 Cl Cl Cl Et Cl I Br Br i-Pr CH3 F Cl Cl i-Pr CH3 Cl Cl Cl i-Pr CI I Br Br t-Bu CH3 F Cl Cl t-Bu CH3 Cl Cl Cl t-Bu Cl I Br Br Me CH3 F Cl Br Me CH3 Cl Cl Br Me Cl CF3 CF3 Cl Et CH3 F Cl Br Et CH3 Cl Cl Br Et Cl CF3 CF3 Cl i-Pr CH3 F Cl Br i-Pr CH3 Cl Cl Br i-Pr Cl CF3 CF3 Cl t-Bu CH3 F Cl Br t-Bu CH3 Cl Cl Br t-Bu Cl CF3 CF3 Cl Me CH3 F Br Cl Me CH3 Cl Br Cl Me CI CF3 CF3 Br Et CH3 F Br Cl Et CH3 Cl Br Cl Et Cl CF3 CF3 Br i-Pr CH3 F Br Cl i-Pr CH3 Cl Br Cl i-Pr Cl CF3 CF3 Br t-Bu CH3 F Br Cl t-Bu CH3 Cl Br Cl t-Bu Cl CF3 CF3 Br Me CH3 F Br Br Me CH3 Cl Br Br Me Cl CF3 Cl Cl Et CH3 F Br Br Et CH3 Cl Br Br Et Cl CF3 Cl Cl i-Pr CH3 F Br Br i-Pr CH3 Cl Br Br i-Pr Cl CF3 Cl Cl t-Bu CH3 F Br Br t-Bu CH3 Cl Br Br t-Bu Cl CF3 Cl Cl Me CH3 Br CF3 Cl Me Cl F CF3 Cl Me Cl CF3 Cl Br Et CH3 Br CF3 Cl Et Cl F CF3 Cl Et Cl CF3 Cl Br i-Pr CH3 Br CF3 Cl i-Pr Cl F CF3 Cl i-Pr Cl CF3 Cl Br t-Bu CH3 Br CF3 Cl t-Bu Cl F CF3 Cl t-Bu Cl CF3 Cl Br Me CH3 Br CF3 Br Me Cl F CF3 Br Me Cl CF3 Br Cl R3 R4a R4b R5 R6 R3 R4a R4b R5 R6 R3 R4a R4b R5 R6 Et CH3 Br CF3 Br Et ci F CF3 Br Et Cl CF3 Br ci i-Pr CH3 Br CF3 Br i-Pr Cl F CF3 Br i-Pr Cl CF3 Br Cl t-Bu CH3 Br CF3 Br t-Bu Cl F CF3 Br t-Bu Cl CF3 Br Cl Me CH3 Br Cl Cl Me Cl F Cl Cl Me Cl CF3 Br Br Et CH3 Br Cl Cl Et Cl F Cl Cl Et Cl CF3 Br Br i-Pr CH3 Br Cl Cl i-Pr Cl F Cl Cl i-Pr Cl CF3 Br Br t-Bu CH3 Br Cl Cl t-Bu Cl F Cl Cl t-Bu Cl CF3 Br Br Me CH3 Br Cl Br Me Cl F Cl Br n-Pr Cl Cl Cl Cl Et CH3 Br Cl Br Et Cl F Cl Br n-Bu Cl Cl Cl Cl i-Pr CH3 Br Cl Br i-Pr Cl F Cl Br s-Bu Cl Cl Cl Cl t-Bu CH3 Br Cl Br t-Bu Cl F Cl Br i-Bu Cl Cl Cl Cl Me CH3 Br Br Cl Me Cl F Br Cl Me Br F CF3 Cl Et CH3 Br Br Cl Et Cl F Br Cl Et Br F CF3 Cl i-Pr CH3 Br Br Cl i-Pr Cl F Br Cl i-Pr Br F CF3 Cl t-Bu CH3 Br Br Cl t-Bu Cl F Br Cl t-Bu Br F CF3 Cl Me CH3 Br Br Br Me Cl F Br Br Me Br F CF3 Br Et CH3 Br Br Br Et Cl F Br Br Et Br F CF3 Br i-Pr CH3 Br Br Br i-Pr Cl F Br Br i-Pr Br F CF3 Br t-Bu CH3 Br Br Br t-Bu Cl F Br Br t-Bu Br F CF3 Br Me CH3 I CF3 Cl Me Cl Cl CF3 Cl Me Br F Cl Cl Et CH3 I CF3 Cl Et Cl Cl CF3 Cl Et Br F Cl Cl i-Pr CH3 I CF3 Cl i-Pr Cl Cl CF3 Cl i-Pr Br F Cl Cl t-Bu CH3 I CF3 Cl t-Bu Cl Cl CF3 Cl t-Bu Br F Cl Cl Me CH3 I CF3 Br Me Cl Cl CF3 Br Me Br F Cl Br Et CH3 I CF3 Br Et Cl Cl CF3 Br Et Br F Cl Br i-Pr CH3 I CF3 Br i-Pr Cl Cl CF3 Br i-Pr Br F Cl Br t-Bu CH3 I CF3 Br t-Bu Cl Cl CF3 Br t-Bu Br F Cl Br Me CH3 I Cl Cl Me Cl Cl Cl Cl Me Br F Br Cl Et CH3 I Cl Cl Et Cl Cl Cl Cl Et Br F Br Cl i-Pr CH3 I Cl Cl i-Pr Cl Cl Cl Cl i-Pr Br F Br Cl t-Bu CH3 I Cl Cl t-Bu Cl Cl Cl Cl t-Bu Br F Br Cl Me CH3 I Cl Br Me Cl Cl Cl Br Me Br F Br Br Et CH3 I Cl Br Et Cl Cl Cl Br Et Br F Br Br i-Pr CH3 I Cl Br i-Pr Cl Cl Cl Br i-Pr Br F Br Br t-Bu CH3 I Cl Br t-Bu Cl Cl Cl Br t-Bu Br F Br Br Me CH3 I Br Cl Me Br CF3 CF3 Cl Me Br Cl CF3 Cl Et CH3 I Br Cl Et Br CF3 CF3 Cl Et Br Cl CF3 Cl R3 R4a R4b R5 R6 R3 R4a R4b R5 R6 R3 R4a R4b R5 R6 i-Pr CH3 I Br Cl i-Pr Br CF3 CF3 Cl i-Pr Br Cl CF3 Cl t-Bu CH3 I Br Cl t-Bu Br CF3 CF3 Cl t-Bu Br Cl CF3 Cl Me CH3 I Br Br Me Br CF3 CF3 Br Me Br Cl CF3 Br Et CH3 I Br Br Et Br CF3 CF3 Br Et Br Cl CF3 Br i-Pr CH3 I Br Br i-Pr Br CF3 CF3 Br i-Pr Br Cl CF3 Br t-Bu CH3 I Br Br t-Bu Br CF3 CF3 Br t-Bu Br Cl CF3 Br Me CH3 CF3 CF3 Cl Me Br CF3 Cl Cl Me Br Cl ci Cl Et CH3 CF3 CF3 Cl Et Br CF3 Cl Cl Et Br Cl Cl Cl i-Pr CH3 CF3 CF3 Cl i-Pr Br CF3 Cl Cl i-Pr Br Cl Cl Cl t-Bu CH3 CF3 CF3 Cl t-Bu Br CF3 Cl Cl t-Bu Br Cl Cl Cl Me CH3 CF3 CF3 Br Me Br CF3 Cl Br Me Br Cl Cl Br Et CH3 CF3 CF3 Br Et Br CF3 Cl Br Et Br Cl Cl Br i-Pr CH3 CF3 CF3 Br i-Pr Br CF3 Cl Br i-Pr Br Cl Cl Br t-Bu CH3 CF3 CF3 Br t-Bu Br CF3 Cl Br t-Bu Br Cl Cl Br Me CH3 CF3 Cl Cl Me Br CF3 Br Cl Me Br Cl Br Cl Et CH3 CF3 Cl Cl Et Br CF3 Br Cl Et Br Cl Br Cl 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I Cl Br i-Pr CH3 F CF3 Cl i-Pr CH3 Cl CF3 Cl i-Pr Cl I Cl Br t-Bu CH3 F CF3 Cl t-Bu CH3 Cl CF3 Cl t-Bu Cl I Cl Br Me CH3 F CF3 Br Me CH3 Cl CF3 Br Me a I Br Cl Et CH3 F CF3 Br Et CH3 Cl CF3 Br Et Cl I Br Cl i-Pr CH3 F CF3 Br i-Pr CH3 Cl CF3 Br i-Pr Cl I Br Cl t-Bu CH3 F CF3 Br t-Bu CH3 Cl CF3 Br t-Bu Cl I Br Cl Me CH3 F Cl Cl Me CH3 Cl Cl Cl Me Cl I Br Br Et CH3 F Cl Cl Et CH3 Cl CI CI Et Cl I Br Br i-Pr CH3 F Cl Cl i-Pr CH3 Cl Cl Cl i-Pr Cl I Br Br t-Bu CH3 F Cl Cl t-Bu CH3 Cl Cl Cl t-Bu Cl I Br Br Me CH3 F Cl Br Me CH3 Cl Cl Br Me Cl CF3 CF3 Cl Et CH3 F Cl Br Et CH3 Cl Cl Br Et Cl CF3 CF3 Cl i-Pr CH3 F Cl Br i-Pr CH3 Cl Cl Br i-Pr Cl CF3 CF3 Cl t-Bu CH3 F Cl Br t-Bu CH3 Cl Cl Br t-Bu Cl CF3 CF3 Cl Me CH3 F Br Cl Me CH3 Cl Br Cl Me Cl CF3 CF3 Br Et CH3 F Br Cl Et CH3 Cl Br Cl Et Cl CF3 CF3 Br i-Pr CH3 F Br Cl i-Pr CH3 Cl Br Cl i-Pr Cl CF3 CF3 Br t-Bu CH3 F Br Cl t-Bu CH3 Cl Br Cl t-Bu Cl CF3 CF3 Br Me CH3 F Br Br Me CH3 Cl Br Br Me Cl CF3 Cl Cl Et CH3 F Br Br Et CH3 Cl Br Br Et Cl CF3 Cl Cl i-Pr CH3 F Br Br i-Pr CH3 Cl Br Br i-Pr Cl CF3 Cl Cl t-Bu CH3 F Br Br t-Bu CH3 Cl Br Br t-Bu Cl CF3 Cl Cl Me CH3 Br CF3 Cl Me Cl F CF3 Cl Me Cl CF3 Cl Br Et CH3 Br CF3 Cl Et Cl F CF3 Cl Et Cl CF3 Cl Br i-Pr CH3 Br CF3 Cl i-Pr Cl F CF3 Cl i-Pr Cl CF3 Cl Br t-Bu CH3 Br CF3 Cl t-Bu Cl F CF3 Cl t-Bu Cl CF3 Cl Br Me CH3 Br CF3 Br Me Cl F CF3 Br Me Cl CF3 Br Cl R3 R4a R4b R5 R6 R3 R4a R4b R5 R6 R3 R4a R4b R5 R6 Et CH3 Br CF3 Br Et Cl F CF3 Br Et Cl CF3 Br Cl i-Pr CH3 Br CF3 Br i-Pr Cl F CF3 Br i-Pr Cl CF3 Br Cl t-Bu CH3 Br CF3 Br t-Bu Cl F CF3 Br t-Bu Cl CF3 Br Cl Me CH3 Br Cl Cl Me Cl F Cl Cl Me Cl CF3 Br Br Et CH3 Br Cl Cl Et ci F Cl Cl Et Cl CF3 Br Br i-Pr CH3 Br Cl Cl i-Pr Cl F Cl Cl i-Pr Cl CF3 Br Br t-Bu CH3 Br Cl Cl t-Bu Cl F Cl Cl t-Bu Cl CF3 Br Br Me CH3 Br Cl Br Me Cl F Cl Br n-Pr Cl CI Cl Cl Et CH3 Br Cl Br Et CI F Cl Br n-Bu Cl Cl Cl Cl i-Pr CH3 Br Cl Br i-Pr Cl F Cl Br s-Bu Cl Cl Cl Cl t-Bu CH3 Br Cl Br t-Bu Cl F Cl Br i-Bu Cl Cl Cl CI Me CH3 Br Br Cl Me Cl F Br Cl Me Br F CF3 Cl Et CH3 Br Br Cl Et CI F Br Cl Et Br F CF3 Cl i-Pr CH3 Br Br Cl i-Pr Cl F Br Cl i-Pr Br F CF3 Cl t-Bu CH3 Br Br Cl t-Bu Cl F Br Cl t-Bu Br F CF3 Cl Me CH3 Br Br Br Me Cl F Br Br Me Br F CF3 Br Et CH3 Br Br Br Et Cl F Br Br Et Br F CF3 Br i-Pr CH3 Br Br Br i-Pr Cl F Br Br i-Pr Br F CF3 Br t-Bu CH3 Br Br Br t-Bu Cl F Br Br t-Bu Br F CF3 Br Me CH3 I CF3 Cl Me Cl Cl CF3 Cl Me Br F Cl Cl Et CH3 I CF3 Cl Et Cl Cl CF3 Cl Et Br F Cl Cl i-Pr CH3 I CF3 Cl i-Pr Cl Cl CF3 Cl i-Pr Br F Cl Cl t-Bu CH3 I CF3 Cl t-Bu Cl Cl CF3 Cl t-Bu Br F Cl Cl Me CH3 I CF3 Br Me Cl Cl CF3 Br Me Br F Cl Br Et CH3 I CF3 Br Et Cl Cl CF3 Br Et Br F Cl Br i-Pr CH3 I CF3 Br i-Pr Cl Cl CF3 Br i-Pr Br F Cl Br t-Bu CH3 I CF3 Br t-Bu Cl Cl CF3 Br t-Bu Br F Cl Br Me CH3 I Cl Cl Me Cl Cl Cl Cl Me Br F Br Cl Et CH3 I Cl Cl Et Cl Cl Cl Cl Et Br F Br Cl i-Pr CH3 I Cl Cl i-Pr Cl Cl Cl Cl i-Pr Br F Br Cl t-Bu CH3 I Cl Cl t-Bu Cl Cl Cl Cl t-Bu Br F Br Cl Me CH3 I Cl Br Me Cl Cl Cl Br Me Br F Br Br Et CH3 I Cl Br Et Cl Cl Cl Br 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Cl Cl Me Br CF3 Br Cl Me Br Cl Br Cl Et CH3 CF3 Cl Cl Et Br CF3 Br Cl Et Br Cl Br Cl i-Pr CH3 CF3 Cl Cl i-Pr Br CF3 Br Cl i-Pr Br Cl Br Cl t-Bu CH3 CF3 Cl Cl t-Bu Br CF3 Br Cl t-Bu Br Cl Br Cl Me CH3 CF3 Cl Br Me Br CF3 Br Br Me Br Cl Br Br Et CH3 CF3 Cl Br Et Br CF3 Br Br Et Br Cl Br Br i-Pr CH3 CF3 Cl Br i-Pr Br CF3 Br Br i-Pr Br Cl Br Br t-Bu CH3 CF3 Cl Br t-Bu Br CF3 Br Br t-Bu Br Cl Br Br Me CH3 CF3 Br Cl Me Br I CF3 Cl Me Br Br CF3 Cl Et CH3 CF3 Br Cl Et Br I CF3 Cl Et Br Br CF3 Cl i-Pr CH3 CF3 Br Cl i-Pr Br I CF3 Cl i-Pr Br Br CF3 Cl t-Bu CH3 CF3 Br Cl t-Bu Br I CF3 Cl t-Bu Br Br CF3 Cl Me CH3 CF3 Br Br Me Br I CF3 Br Me Br Br CF3 Br Et CH3 CF3 Br Br Et Br I CF3 Br Et Br Br CF3 Br i-Pr CH3 CF3 Br Br i-Pr Br I CF3 Br i-Pr Br Br CF3 Br t-Bu CH3 CF3 Br Br t-Bu Br I CF3 Br t-Bu Br Br CF3 Br n-Pr CH3 Cl Cl Cl Me Br I Cl Cl Me Br Br Cl Ci n-Bu CH3 Cl Cl Cl Et Br I Cl Cl Et Br Br Cl Cl s-Bu CH3 Cl Cl Cl i-Pr Br I Cl Cl i-Pr Br Br Cl Cl i-Bu CH3 Cl Cl Cl t-Bu Br I Cl Cl t-Bu Br Br Cl Cl Me Cl Cl Br Cl Me Br I Cl Br Me Br Br Cl Br Et Cl Cl Br Cl Et Br I Cl Br Et Br Br Cl Br i-Pr Cl Cl Br Cl i-Pr Br I Cl Br i-Pr Br Br Cl Br R3 R4a R4b R5 R6 R3 R4a R4b R5 R6 R3 R4a R4b R5 R6 t-Bu Cl Cl Br Cl t-Bu Br I Cl Br t-Bu Br Br Cl Br Me Cl Cl Br Br Me Br I Br Cl Me Br Br Br Cl Et Cl Cl Br Br Et Br I Br Cl Et Br Br Br CI i-Pr Cl Cl Br Br i-Pr Br I Br Cl i-Pr Br Br Br Cl t-Bu Cl Cl Br Br t-Bu Br I Br Cl t-Bu Br Br Br Cl Me Cl Br CF3 Cl Me Br I Br Br Me Br Br Br Br Et Cl Br CF3 Cl Et Br I Br Br Et Br Br Br Br i-Pr Cl Br CF3 Cl i-Pr Br I Br Br i-Pr Br Br Br Br t-Bu Cl Br CF3 Cl t-Bu Br I Br Br t-Bu Br Br Br Br Me Cl Br CF3 Br Me Cl Br Cl Cl t-Bu Cl Br CF3 Br Et Cl Br CF3 Br Et Cl Br Cl Cl t-Bu Cl Br Cl Cl i-Pr Cl Br CF3 Br i-Pr Cl Br Cl Cl Table S R3 R4a R4b R5 R6 R3 R4a R4b R5 R6 R3 R4a R4b R5 R6 Me CH3 H CF3 Cl Me Cl H Cl Br Me Cl Br Cl Br Et CH3 H CF3 Cl Et Cl H Cl Br Et Cl Br Cl Br i-Pr CH3 H CF3 Cl i-Pr Cl H Cl Br i-Pr Cl Br Cl Br t-Bu CH3 H CF3 Cl t-Bu Cl H Cl Br t-Bu Cl Br Cl Br Me CH3 H CF3 Br Me Cl H Br Cl Me Cl Br Br CI Et CH3 H CF3 Br Et Cl H Br Cl Et Cl Br Br Cl i-Pr CH3 H CF3 Br i-Pr Cl H Br Cl i-Pr Cl Br Br Cl t-Bu CH3 H CF3 Br t-Bu Cl H Br Cl t-Bu Cl Br Br CI Me CH3 H Cl Cl Me Cl H Br Br Me Cl Br Br Br Et CH3 H Cl Cl Et Cl H Br Br Et Cl Br Br Br i-Pr CH3 H Cl Cl i-Pr Cl H Br Br i-Pr Cl Br Br Br t-Bu CH3 H Cl Cl t-Bu Cl H Br Br t-Bu Cl Br Br Br Me CH3 H Cl Br Me Cl H CF3 Cl Me Cl I CF3 Cl Et CH3 H Cl Br Et Cl H CF3 Cl Et Cl I CF3 Cl i-Pr CH3 H Cl Br i-Pr Cl H CF3 Cl i-Pr Cl I CF3 Cl t-Bu CH3 H Cl Br t-Bu Cl H CF3 Cl t-Bu Cl I CF3 Cl R3 R4a R4b R5 R6 R3 R4a R4b R5 R6 R3 R4a R4b R5 R6 Me CH3 H Br Cl Me Cl H CF3 Br Me Cl I CF3 Br Et CH3 H Br Cl Et Cl H CF3 Br Et Cl I CF3 Br i-Pr CH3 H Br Cl i-Pr Cl H CF3 Br i-Pr Cl I CF3 Br t-Bu CH3 H Br Cl t-Bu Cl H CF3 Br t-Bu Cl I CF3 Br Me CH3 H Br Br Me Cl H Cl Cl Me Cl I Cl Cl Et CH3 H Br Br Et Cl H Cl Cl Et ci I ci ci i-Pr CH3 H Br Br i-Pr Cl H Cl Cl i-Pr Cl I Cl Cl t-Bu CH3 H Br Br i-Pr Cl H Cl Cl t-Bu Cl I Cl Cl Me CH3 F CF3 Cl Me CH3 Cl CF3 Cl Me Cl I Cl Br Et CH3 F CF3 Cl Et CH3 Cl CF3 Cl Et Cl I Cl Br i-Pr CH3 F CF3 Cl i-Pr CH3 Cl CF3 Cl i-Pr CI I Cl Br t-Bu CH3 F CF3 Cl t-Bu CH3 Cl CF3 Cl t-Bu Cl I Cl Br Me CH3 F CF3 Br Me CH3 Cl CF3 Br Me Cl I Br Cl Et CH3 F CF3 Br Et CH3 Cl CF3 Br Et Cl I Br Cl i-Pr CH3 F CF3 Br i-Pr CH3 Cl CF3 Br i-Pr Cl I Br Cl t-Bu CH3 F CF3 Br t-Bu CH3 Cl CF3 Br t-Bu Cl I Br Cl Me CH3 F Cl Cl Me CH3 Cl Cl Cl Me Cl I Br Br Et CH3 F Cl Cl Et CH3 Cl Cl Cl Et Cl I Br Br i-Pr CH3 F Cl Cl i-Pr CH3 Cl Cl Cl i-Pr Cl I Br Br t-Bu CH3 F Cl Cl t-Bu CH3 Cl Cl Cl t-Bu Cl I Br Br Me CH3 F Cl Br Me CH3 Cl Cl Br Me Cl CF3 CF3 Cl Et CH3 F Cl Br Et CH3 Cl Cl Br Et Cl CF3 CF3 Cl i-Pr CH3 F Cl Br i-Pr CH3 Cl Cl Br i-Pr Cl CF3 CF3 Cl t-Bu CH3 F Cl Br t-Bu CH3 Cl Cl Br t-Bu Cl CF3 CF3 Cl Me CH3 F Br Cl Me CH3 Cl Br Cl Me Cl CF3 CF3 Br Et CH3 F Br Cl Et CH3 Cl Br Cl Et Cl CF3 CF3 Br i-Pr CH3 F Br Cl i-Pr CH3 Cl Br Cl i-Pr Cl CF3 CF3 Br t-Bu CH3 F Br Cl t-Bu CH3 Cl Br Cl t-Bu Cl CF3 CF3 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Cl t-Bu Br CF3 CF3 Br t-Bu Br F Cl Cl Me CH3 I CF3 Br Me Br CF3 Cl Cl Me Br F Cl Br Et CH3 I CF3 Br Et Br CF3 Cl Cl Et Br F Cl Br i-Pr CH3 I CF3 Br i-Pr Br CF3 Cl Cl i-Pr Br F Cl Br t-Bu CH3 I CF3 Br t-Bu Br CF3 Cl Cl t-Bu Br F Cl Br Me CH3 I Cl Cl Me Br CF3 Cl Br Me Br F Br Cl Et CH3 I Cl Cl Et Br CF3 Cl Br Et Br F Br Cl i-Pr CH3 I Cl Cl i-Pr Br CF3 Cl Br i-Pr Br F Br Cl t-Bu CH3 I Cl Cl t-Bu Br CF3 Cl Br t-Bu Br F Br CI Me CH3 I Cl Br Me Br CF3 Br Cl Me Br F Br Br Et CH3 I Cl Br Et Br CF3 Br Cl Et Br F Br Br i-Pr CH3 I Cl Br i-Pr Br CF3 Br Cl i-Pr Br F Br Br t-Bu CH3 I Cl Br t-Bu Br CF3 Br Cl t-Bu Br F Br Br Me CH3 I Br Cl Me Br CF3 Br Br Me Br Cl CF3 Cl Et CH3 I Br Cl Et Br CF3 Br Br Et Br Cl CF3 Cl i-Pr CH3 I Br Cl i-Pr Br CF3 Br Br i-Pr Br Cl CF3 Cl t-Bu CH3 I Br Cl t-Bu Br CF3 Br Br t-Bu Br Cl CF3 Cl Me CH3 I Br Br Me Br Br CF3 Cl Me Br Cl CF3 Br Et CH3 I Br Br Et Br Br CF3 Cl Et Br Cl CF3 Br i-Pr CH3 I Br Br i-Pr Br Br CF3 Cl i-Pr Br Cl CF3 Br t-Bu CH3 I Br Br t-Bu Br Br CF3 Cl t-Bu Br Cl CF3 Br Me CH3 CF3 CF3 Cl Me Br Br CF3 Br Me Br Cl CI Cl Et CH3 CF3 CF3 Cl Et Br Br CF3 Br Et Br Cl CI Cl i-Pr CH3 CF3 CF3 Cl i-Pr Br Br CF3 Br i-Pr Br Cl Cl Cl t-Bu CH3 CF3 CF3 Cl t-Bu Br Br CF3 Br t-Bu Br Cl Cl Cl Me CH3 CF3 CF3 Br Me Br Br Cl Cl Me Br Cl Cl Br Et CH3 CF3 CF3 Br Et Br Br Cl Cl Et Br Cl Cl Br R3 R4a R4b R5 R6 R3 R4a R4b R5 R6 R3 R4a R4b R5 R6 i-Pr CH3 CF3 CF3 Br i-Pr Br Br Cl Cl i-Pr Br Cl Cl Br t-Bu CH3 CF3 CF3 Br t-Bu Br Br Cl Cl t-Bu Br Cl Cl Br Me CH3 CF3 Cl Cl Me Br Br Cl Br Me Br Cl Br Cl Et CH3 CF3 Cl Cl Et Br Br Cl Br Et Br Cl Br Cl i-Pr CH3 CF3 Cl Cl i-Pr Br Br Cl Br i-Pr Br Cl Br Cl t-Bu CH3 CF3 Cl Cl t-Bu Br Br Cl Br t-Bu Br Cl Br Cl Me CH3 CF3 Cl Br Me CH3 CF3 Br Cl Me Br Cl Br Br Et CH3 CF3 Cl Br Et CH3 CF3 Br Cl Et Br Cl Br Br i-Pr CH3 CF3 Cl Br i-Pr CH3 CF3 Br Cl i-Pr Br Cl Br Br t-Bu CH3 CF3 Cl Br t-Bu CH3 CF3 Br Cl t-Bu Br Cl Br Br Me CH3 CF3 Br Br n-Pr CH3 Cl Cl Cl t-Bu CH3 CF3 Br Br Et CH3 CF3 Br Br n-Bu CH3 Cl Cl Cl i-Bu CH3 Cl Cl Cl i-Pr CH3 CF3 Br Br s-Bu CH3 Cl Cl Cl Table 11 R3 R4a R4b R5 R6 R3 R4a R4b R5 R6 R3 R4a R4b R5 R6 Me CH3 H CF3 Cl Me Cl F CF3 Cl Me Cl H Cl Br Et CH3 H CF3 Cl Et Cl F CF3 Cl Et Cl H Cl Br i-Pr CH3 H CF3 Cl i-Pr Cl F CF3 Cl i-Pr Cl H Cl Br t-Bu CH3 H CF3 Cl t-Bu Cl F CF3 Cl t-Bu Cl H Cl Br Me CH3 H CF3 Br Me Cl F CF3 Br Me Cl H Br CI Et CH3 H CF3 Br Et Cl F CF3 Br Et Cl H Br Cl i-Pr CH3 H CF3 Br i-Pr Cl F CF3 Br i-Pr Cl H Br Cl t-Bu CH3 H CF3 Br t-Bu Cl F CF3 Br t-Bu Cl H Br Cl Me CH3 H Cl Cl Me Cl F Cl Cl Me Cl H Br Br Et CH3 H Cl Cl Et Cl F Cl Cl Et Cl H Br Br i-Pr CH3 H Cl Cl i-Pr Cl F Cl Cl i-Pr Cl H Br Br t-Bu CH3 H Cl Cl t-Bu Cl F Cl Cl t-Bu Cl H Br Br Me CH3 H Cl Br Me Cl F Cl Br Me Cl H CF3 Cl Et CH3 H Cl Br Et CI F Cl Br Et Cl H CF3 Cl i-Pr CH3 H Cl Br i-Pr Cl F Cl Br i-Pr Cl H CF3 Cl R3 R4a R4b R5 R6 R3 R4a R4b R5 R6 R3 R4a R4b R5 R6 t-Bu CH3 H Cl Br t-Bu Cl F Cl Br t-Bu Cl H CF3 Cl Me CH3 H Br Cl Me Cl F Br Cl Me Cl H CF3 Br Et CH3 H Br Cl Et Cl F Br Cl Et Cl H CF3 Br i-Pr CH3 H Br Cl i-Pr Cl F Br Cl i-Pr Cl H CF3 Br t-Bu CH3 H Br Cl t-Bu Cl F Br Cl t-Bu Cl H CF3 Br Me CH3 H Br Br Me Cl F Br Br Me Cl H Cl Cl Et CH3 H Br Br Et Cl F Br Br Et Cl H Cl Cl i-Pr CH3 H Br Br i-Pr Cl F Br Br i-Pr Cl H Cl Cl t-Bu CH3 H Br Br t-Bu Cl F Br Br i-Pr Cl H Cl Cl Me CH3 F CF3 Cl Me Cl Cl CF3 Cl Me Cl Br Cl Br Et CH3 F CF3 Cl Et Cl Cl CF3 Cl Et Cl Br Cl Br i-Pr CH3 F CF3 Cl i-Pr Cl Cl CF3 Cl i-Pr Cl Br Cl Br t-Bu CH3 F CF3 Cl t-Bu Cl Cl CF3 Cl t-Bu Cl Br Cl Br Me CH3 F CF3 Br Me Cl Cl CF3 Br Me Cl Br Br Cl Et CH3 F CF3 Br Et Cl Cl CF3 Br Et Cl Br Br Cl i-Pr CH3 F CF3 Br i-Pr Cl Cl CF3 Br i-Pr Cl Br Br CI t-Bu CH3 F CF3 Br t-Bu Cl Cl CF3 Br t-Bu Cl Br Br Cl Me CH3 F Cl Cl Me Cl Cl Cl Cl Me Cl Br Br Br Et CH3 F Cl Cl Et Cl Cl Cl Cl Et Cl Br Br Br i-Pr CH3 F Cl Cl i-Pr Cl Cl Cl Cl i-Pr Cl Br Br Br t-Bu CH3 F Cl Cl t-Bu Cl Cl Cl Cl t-Bu Cl Br Br Br Me CH3 F Cl Br Me Cl Cl Cl Br Me Cl I CF3 Cl Et CH3 F Cl Br Et Cl Cl Cl Br Et Cl I CF3 Cl i-Pr CH3 F Cl Br i-Pr Cl Cl Cl Br i-Pr Cl I CF3 Cl t-Bu CH3 F Cl Br t-Bu Cl Cl Cl Br t-Bu Cl I CF3 Cl Me CH3 F Br Cl Me Cl Cl Br Cl Me Cl I CF3 Br Et CH3 F Br Cl Et Cl CI Br Cl Et Cl I CF3 Br i-Pr CH3 F Br Cl i-Pr Cl Cl Br Cl i-Pr Cl I CF3 Br t-Bu CH3 F Br Cl t-Bu Cl Cl Br Cl t-Bu Cl I CF3 Br Me CH3 F Br Br Me Cl Cl Br Br Me Cl I Cl Cl Et CH3 F Br Br Et Cl Cl Br Br Et Cl I Cl Cl i-Pr CH3 F Br Br i-Pr Cl Cl Br Br i-Pr Cl I Cl Cl t-Bu CH3 F Br Br t-Bu Cl Cl Br Br t-Bu Cl I Cl Cl Me CH3 Cl CF3 Cl Me Cl Br CF3 Cl Me Cl I Cl Br Et CH3 Cl CF3 Cl Et Cl Br CF3 Cl Et Cl I Cl Br i-Pr CH3 Cl CF3 Cl i-Pr Cl Br CF3 Cl i-Pr Cl I Cl Br t-Bu CH3 Cl CF3 Cl t-Bu Cl Br CF3 Cl t-Bu Cl I Cl Br R3 R4a R4b R5 R6 R3 R4a R4b R5 R6 R3 R4a R4b R5 R6 Me CH3 Cl CF3 Br Me Cl Br CF3 Br Me Cl I Br Cl Et CH3 Cl CF3 Br Et Cl Br CF3 Br Et Cl I Br Cl i-Pr CH3 Cl CF3 Br i-Pr Cl Br CF3 Br i-Pr Cl I Br Cl t-Bu CH3 Cl CF3 Br t-Bu Cl Br CF3 Br t-Bu Cl I Br CI Me CH3 Cl Cl Cl Me Cl Br Cl Cl Me Cl I Br Br Et CH3 Cl Cl Cl Et Cl Br Cl Cl Et Cl I Br Br i-Pr CH3 Cl Cl Cl i-Pr Cl Br Cl Cl i-Pr Cl I Br Br t-Bu CH3 Cl Cl Cl t-Bu Cl Br Cl Cl t-Bu Cl I Br Br Me CH3 Cl Cl Br Me Br Br Br Cl Me Cl CF3 CF3 Cl Et CH3 Cl Cl Br Et Br Br Br Cl Et Cl CF3 CF3 Cl i-Pr CH3 Cl Cl Br i-Pr Br Br Br Cl i-Pr Cl CF3 CF3 Cl t-Bu CH3 Cl Cl Br t-Bu Br Br Br Cl t-Bu Cl CF3 CF3 Cl Me CH3 Cl Br Cl Me Br Br Br Br Me Cl CF3 CF3 Br Et CH3 Cl Br Cl Et Br Br Br Br Et Cl CF3 CF3 Br i-Pr CH3 Cl Br Cl i-Pr Br Br Br Br i-Pr Cl CF3 CF3 Br t-Bu CH3 Cl Br Cl t-Bu Br Br Br Br t-Bu Cl CF3 CF3 Br Me CH3 Cl Br Br Me Br I CF3 Cl Me Cl CF3 Cl Cl Et CH3 Cl Br Br Et Br I CF3 Cl Et Cl CF3 Cl Cl i-Pr CH3 Cl Br Br i-Pr Br I CF3 Cl i-Pr Cl CF3 Cl Cl t-Bu CH3 Cl Br Br t-Bu Br I CF3 Cl t-Bu Cl CF3 Cl Cl Me CH3 Br CF3 Cl Me Br I CF3 Br Me Cl CF3 Cl Br Et CH3 Br CF3 Cl Et Br I CF3 Br Et Cl CF3 Cl Br i-Pr CH3 Br CF3 Cl i-Pr Br I CF3 Br i-Pr Cl CF3 Cl Br t-Bu CH3 Br CF3 Cl t-Bu Br I CF3 Br t-Bu Cl CF3 Cl Br Me CH3 Br CF3 Br Me Br I Cl Cl Me Cl CF3 Br Cl Et CH3 Br CF3 Br Et Br I Cl Cl Et Cl CF3 Br Cl i-Pr CH3 Br CF3 Br i-Pr Br I Cl Cl i-Pr Cl CF3 Br Cl t-Bu CH3 Br CF3 Br t-Bu Br I Cl Cl t-Bu Cl CF3 Br Cl Me CH3 Br Cl Cl Me Br I Cl Br Me Cl CF3 Br Br Et CH3 Br Cl Cl Et Br I Cl Br Et Cl CF3 Br Br i-Pr CH3 Br Cl Cl i-Pr Br I Cl Br i-Pr Cl CF3 Br Br t-Bu CH3 Br Cl Cl t-Bu Br I Cl Br t-Bu Cl CF3 Br Br Me CH3 Br Cl Br Me Br I Br Cl n-Pr Cl Cl Cl Cl Et CH3 Br Cl Br Et Br I Br Cl n-Bu Cl Cl Cl Cl i-Pr CH3 Br Cl Br i-Pr Br I Br Cl s-Bu Cl Cl Cl CI t-Bu CH3 Br Cl Br t-Bu Br I Br Cl i-Bu Cl Cl Cl Cl Me CH3 Br Br Cl Me Br I Br Br Me Br F CF3 Cl R3 R4a R4b R5 R6 R3 R4a R4b R5 R6 R3 R4a R4b R5 R6 Et CH3 Br Br Cl Et Br I Br Br Et Br F CF3 Cl i-Pr CH3 Br Br Cl i-Pr Br I Br Br i-Pr Br F CF3 Cl t-Bu CH3 Br Br Cl t-Bu Br I Br Br t-Bu Br F CF3 Cl Me CH3 Br Br Br Me Br CF3 CF3 Cl Me Br F CF3 Br Et CH3 Br Br Br Et Br CF3 CF3 Cl Et Br F CF3 Br i-Pr CH3 Br Br Br i-Pr Br CF3 CF3 Cl i-Pr Br F CF3 Br t-Bu CH3 Br Br Br t-Bu Br CF3 CF3 Cl t-Bu Br F CF3 Br Me CH3 I CF3 Cl Me Br CF3 CF3 Br Me Br F Cl Cl Et CH3 I CF3 Cl Et Br CF3 CF3 Br Et Br F Cl Cl i-Pr CH3 I CF3 Cl i-Pr Br CF3 CF3 Br i-Pr Br F Cl CI t-Bu CH3 I CF3 Cl t-Bu Br CF3 CF3 Br t-Bu Br F Cl Cl Me CH3 I CF3 Br Me Br CF3 Cl Cl Me Br F Cl Br Et CH3 I CF3 Br Et Br CF3 Cl Cl Et Br F Cl Br i-Pr CH3 I CF3 Br i-Pr Br CF3 Cl Cl i-Pr Br F Cl Br t-Bu CH3 I CF3 Br t-Bu Br CF3 Cl Cl t-Bu Br F Cl Br Me CH3 I Cl Cl Me Br CF3 Cl Br Me Br F Br Cl Et CH3 I Cl Cl Et Br CF3 Cl Br Et Br F Br Cl i-Pr CH3 I Cl Cl i-Pr Br CF3 Cl Br i-Pr Br F Br Cl t-Bu CH3 I Cl Cl t-Bu Br CF3 Cl Br t-Bu Br F Br Cl Me CH3 I Cl Br Me Br CF3 Br Cl Me Br F Br Br Et CH3 I Cl Br Et Br CF3 Br Cl Et Br F Br Br i-Pr CH3 I Cl Br i-Pr Br CF3 Br Cl i-Pr Br F Br Br t-Bu CH3 I Cl Br t-Bu Br CF3 Br Cl t-Bu Br F Br Br Me CH3 I Br Cl Me Br CF3 Br Br Me Br Cl CF3 Cl Et CH3 I Br Cl Et Br CF3 Br Br Et Br Cl CF3 Cl i-Pr CH3 I Br Cl i-Pr Br CF3 Br Br i-Pr Br Cl CF3 Cl t-Bu CH3 I Br Cl t-Bu Br CF3 Br Br t-Bu Br Cl CF3 Cl Me CH3 I Br Br Me Br Br CF3 Cl Me Br Cl CF3 Br Et CH3 I Br Br Et Br Br CF3 Cl Et Br Cl CF3 Br i-Pr CH3 I Br Br i-Pr Br Br CF3 Cl i-Pr Br Cl CF3 Br t-Bu CH3 I Br Br t-Bu Br Br CF3 Cl t-Bu Br Cl CF3 Br Me CH3 CF3 CF3 Cl Me Br Br CF3 Br Me Br Cl Cl Cl Et CH3 CF3 CF3 Cl Et Br Br CF3 Br Et Br ci Cl Cl i-Pr CH3 CF3 CF3 Cl i-Pr Br Br CF3 Br i-Pr Br Cl Cl Cl t-Bu CH3 CF3 CF3 Cl t-Bu Br Br CF3 Br t-Bu Br Cl Cl Cl Me CH3 CF3 CF3 Br Me Br Br Cl Cl Me Br Cl Cl Br Et CH3 CF3 CF3 Br Et Br Br Cl Cl Et Br Cl Cl Br R3 R4a R4b R5 R6 R3 R4a R4b R5 R6 R3 R4a R4b R5 R6 i-Pr CH3 CF3 CF3 Br i-Pr Br Br Cl Cl i-Pr Br Cl Cl Br t-Bu CH3 CF3 CF3 Br t-Bu Br Br Cl Cl t-Bu Br Cl Cl Br Me CH3 CF3 Cl Cl Me Br Br Cl Br Me Br Cl Br Cl Et CH3 CF3 Cl Cl Et Br Br Cl Br Et Br Cl Br Cl i-Pr CH3 CF3 Cl Cl i-Pr Br Br Cl Br i-Pr Br Cl Br Cl t-Bu CH3 CF3 Cl Cl t-Bu Br Br Cl Br t-Bu Br Cl Br Cl Me CH3 CF3 Cl Br Me CH3 CF3 Br Cl Me Br Cl Br Br Et CH3 CF3 Cl Br Et CH3 CF3 Br Cl Et Br Cl Br Br i-Pr CH3 CF3 Cl Br i-Pr CH3 CF3 Br Cl i-Pr Br Cl Br Br t-Bu CH3 CF3 Cl Br t-Bu CH3 CF3 Br Cl t-Bu Br Cl Br Br Me CH3 CF3 Br Br n-Pr CH3 Cl Cl Cl t-Bu CH3 CF3 Br Br Et CH3 CF3 Br Br n-Bu CH3 Cl Cl Cl i-Bu CH3 Cl Cl Cl i-Pr CH3 CF3 Br Br s-Bu CH3 Cl Cl Cl Table 12 R3 R4a R4b R5 R6 R3 R4a R4b R5 R6 R3 R4a R4b R5 R6 Me CH3 H CF3 Cl Me Cl F CF3 Cl Me Cl H Cl Br Et CH3 H CF3 Cl Et Ci F CF3 Cl Et Cl H Cl Br i-Pr CH3 H CF3 Cl i-Pr Cl F CF3 Cl i-Pr Cl H Cl Br t-Bu CH3 H CF3 Cl t-Bu Cl F CF3 Cl t-Bu Cl H Cl Br Me CH3 H CF3 Br Me Cl F CF3 Br Me Cl H Br Cl Et CH3 H CF3 Br Et Cl F CF3 Br Et CI H Br Cl i-Pr CH3 H CF3 Br i-Pr Cl F CF3 Br i-Pr CI H Br Cl t-Bu CH3 H CF3 Br t-Bu Cl F CF3 Br t-Bu Cl H Br Cl Me CH3 H Cl Cl Me Cl F Cl Cl Me Cl H Br Br Et CH3 H Cl Cl Et CI F Cl Cl Et ci H Br Br i-Pr CH3 H Cl Cl i-Pr Cl F Cl Cl i-Pr Cl H Br Br t-Bu CH3 H Cl Cl t-Bu Cl F Cl Cl t-Bu Cl H Br Br Me CH3 H Cl Br Me Cl F Cl Br Me Cl H CF3 Cl Et CH3 H Cl Br Et Cl F Cl Br Et ci H CF3 Cl R3 R4a R4b R5 R6 R3 R4a R4b R5 R6 R3 R4a R4b R5 R6 i-Pr CH3 H Cl Br i-Pr Cl F Cl Br i-Pr Cl H CF3 Cl t-Bu CH3 H Cl Br t-Bu Cl F Cl Br t-Bu Cl H CF3 Cl Me CH3 H Br Cl Me Cl F Br Cl Me Cl H CF3 Br Et CH3 H Br Cl Et Cl F Br Cl Et Cl H CF3 Br i-Pr CH3 H Br Cl i-Pr Cl F Br Cl i-Pr Cl H CF3 Br t-Bu CH3 H Br Cl t-Bu Cl F Br Cl t-Bu Cl H CF3 Br Me CH3 H Br Br Me Cl F Br Br Me Cl H Cl Cl Et CH3 H Br Br Et Cl F Br Br Et Cl H Cl Cl i-Pr CH3 H Br Br i-Pr Cl F Br Br i-Pr Cl H Cl Cl t-Bu CH3 H Br Br t-Bu Cl F Br Br i-Pr Cl H Cl Cl Me CH3 F CF3 Cl Me Cl Cl CF3 Cl Me Cl Br Cl Br Et CH3 F CF3 Cl Et Cl Cl CF3 Cl Et Cl Br Cl Br i-Pr CH3 F CF3 Cl i-Pr Cl Cl CF3 Cl i-Pr Cl Br Cl Br t-Bu CH3 F CF3 Cl t-Bu Cl Cl CF3 Cl t-Bu Cl Br Cl Br Me CH3 F CF3 Br Me Cl Cl CF3 Br Me Cl Br Br Cl Et CH3 F CF3 Br Et Cl Cl CF3 Br Et Cl Br Br Cl i-Pr CH3 F CF3 Br i-Pr Cl Cl CF3 Br i-Pr Cl Br Br Cl t-Bu CH3 F CF3 Br t-Bu Cl Cl CF3 Br t-Bu Cl Br Br Cl Me CH3 F Cl Cl Me Cl Cl Cl Cl Me Cl Br Br Br Et CH3 F Cl Cl Et Cl Cl Cl CI Et Cl Br Br Br i-Pr CH3 F Cl Cl i-Pr Cl Cl Cl Cl i-Pr Cl Br Br Br t-Bu CH3 F Cl Cl t-Bu Cl Cl Cl Cl t-Bu Cl Br Br Br Me CH3 F Cl Br Me Cl Cl Cl Br Me CI I CF3 Cl Et CH3 F Cl Br Et Cl Cl Cl Br Et Cl I CF3 Cl i-Pr CH3 F Cl Br i-Pr Cl Cl Cl Br i-Pr Cl I CF3 Cl t-Bu CH3 F Cl Br t-Bu Cl Cl Cl Br t-Bu Cl I CF3 Cl Me CH3 F Br Cl Me Cl CI Br Cl Me Cl I CF3 Br Et CH3 F Br Cl Et Cl Cl Br Cl Et Cl I CF3 Br i-Pr CH3 F Br Cl i-Pr Cl Cl Br Cl i-Pr Cl I CF3 Br t-Bu CH3 F Br Cl t-Bu Cl Cl Br Cl t-Bu Cl I CF3 Br Me CH3 F Br Br Me Cl Cl Br Br Me Cl I Cl Cl Et CH3 F Br Br Et Cl Cl Br Br Et Cl I CI Cl i-Pr CH3 F Br Br i-Pr Cl Cl Br Br i-Pr Cl I Cl Cl t-Bu CH3 F Br Br t-Bu Cl Cl Br Br t-Bu Cl I Cl Cl Me CH3 Cl CF3 Cl Me Cl Br CF3 Cl Me Cl I Cl Br Et CH3 Cl CF3 Cl Et Cl Br CF3 Cl Et Cl I Cl Br i-Pr CH3 Cl CF3 Cl i-Pr Cl Br CF3 Cl i-Pr Cl I Cl Br R3 R4a R4b R5 R6 R3 R4a R4b R5 R6 R3 R4a R4b R5 R6 t-Bu CH3 Cl CF3 Cl t-Bu Cl Br CF3 Cl t-Bu Cl I Cl Br Me CH3 Cl CF3 Br Me Cl Br CF3 Br Me Cl I Br Cl Et CH3 Cl CF3 Br Et Cl Br CF3 Br Et Cl I Br Cl i-Pr CH3 Cl CF3 Br i-Pr Cl Br CF3 Br i-Pr Cl I Br Cl t-Bu CH3 Cl CF3 Br t-Bu Cl Br CF3 Br t-Bu Cl I Br Cl Me CH3 Cl Cl Cl Me Cl Br Cl Cl Me Cl I Br Br Et CH3 Cl Cl Cl Et Cl Br Cl Cl Et Cl I Br Br i-Pr CH3 Cl Cl Cl i-Pr Cl Br Cl Cl i-Pr Cl I Br Br t-Bu CH3 Cl Cl Cl t-Bu Cl Br Cl Cl t-Bu Cl I Br Br Me CH3 Cl Cl Br Me Br Br Br Cl Me Cl CF3 CF3 Cl Et CH3 Cl Cl Br Et Br Br Br Cl Et Cl CF3 CF3 Cl i-Pr CH3 Cl Cl Br i-Pr Br Br Br Cl i-Pr Cl CF3 CF3 Cl t-Bu CH3 Cl Cl Br t-Bu Br Br Br Cl t-Bu Cl CF3 CF3 Cl Me CH3 Cl Br Cl Me Br Br Br Br Me Cl CF3 CF3 Br Et CH3 Cl Br Cl Et Br Br Br Br Et Cl CF3 CF3 Br i-Pr CH3 Cl Br Cl i-Pr Br Br Br Br i-Pr Cl CF3 CF3 Br t-Bu CH3 Cl Br Cl t-Bu Br Br Br Br t-Bu Cl CF3 CF3 Br Me CH3 Cl Br Br Me Br I CF3 Cl Me Cl CF3 Cl Cl Et CH3 Cl Br Br Et Br I CF3 Cl Et Cl CF3 Cl Cl i-Pr CH3 Cl Br Br i-Pr Br I CF3 Cl i-Pr Cl CF3 Cl Cl t-Bu CH3 Cl Br Br t-Bu Br I CF3 Cl t-Bu Cl CF3 Cl Cl Me CH3 Br CF3 Cl Me Br I CF3 Br Me Cl CF3 Cl Br Et CH3 Br CF3 Cl Et Br I CF3 Br Et Cl CF3 Cl Br i-Pr CH3 Br CF3 Cl i-Pr Br I CF3 Br i-Pr Cl CF3 Cl Br t-Bu CH3 Br CF3 Cl t-Bu Br I CF3 Br t-Bu Cl CF3 Cl Br Me CH3 Br CF3 Br Me Br I Cl Cl Me Cl CF3 Br Cl Et CH3 Br CF3 Br Et Br I Cl Cl Et Cl CF3 Br Cl i-Pr CH3 Br CF3 Br i-Pr Br I Cl Cl i-Pr Cl CF3 Br Cl t-Bu CH3 Br CF3 Br t-Bu Br I Cl Cl t-Bu Cl CF3 Br Cl Me CH3 Br Cl Cl Me Br I Cl Br Me Cl CF3 Br Br Et CH3 Br Cl Cl Et Br I Cl Br Et Cl CF3 Br Br i-Pr CH3 Br Cl Cl i-Pr Br I Cl Br i-Pr Cl CF3 Br Br t-Bu CH3 Br Cl CI t-Bu Br I Cl Br t-Bu Cl CF3 Br Br Me CH3 Br Cl Br Me Br I Br Cl n-Pr Cl Cl CI CI Et CH3 Br Cl Br Et Br I Br Cl zt-Bu Cl Cl Cl Cl i-Pr CH3 Br Cl Br i-Pr Br I Br Cl s-Bu Cl Cl CI Cl t-Bu CH3 Br Cl Br t-Bu Br I Br Cl i-Bu Cl Cl Cl Cl R3 R4a R4b R5 R6 R3 R4a R4b R5 R6 R3 R4a R4b R5 R6 Me CH3 Br Br Cl Me Br I Br Br Me Br F CF3 Cl Et CH3 Br Br Cl Et Br I Br Br Et Br F CF3 Cl i-Pr CH3 Br Br Cl i-Pr Br I Br Br i-Pr Br F CF3 Cl t-Bu CH3 Br Br Cl t-Bu Br I Br Br t-Bu Br F CF3 Cl Me CH3 Br Br Br Me Br CF3 CF3 Cl Me Br F CF3 Br Et CH3 Br Br Br Et Br CF3 CF3 Cl Et Br F CF3 Br i-Pr CH3 Br Br Br i-Pr Br CF3 CF3 Cl i-Pr Br F CF3 Br t-Bu CH3 Br Br Br t-Bu Br CF3 CF3 Cl t-Bu Br F CF3 Br Me CH3 I CF3 Cl Me Br CF3 CF3 Br Me Br F Cl CI Et CH3 I CF3 Cl Et Br CF3 CF3 Br Et Br F Cl Cl i-Pr CH3 I CF3 Cl i-Pr Br CF3 CF3 Br i-Pr Br F Cl Cl t-Bu CH3 I CF3 Cl t-Bu Br CF3 CF3 Br t-Bu Br F Cl Cl Me CH3 I CF3 Br Me Br CF3 Cl Cl Me Br F Cl Br Et CH3 I CF3 Br Et Br CF3 Cl Cl Et Br F Cl Br i-Pr CH3 I CF3 Br i-Pr Br CF3 Cl Cl i-Pr Br F Cl Br t-Bu CH3 I CF3 Br t-Bu Br CF3 Cl Cl t-Bu Br F Cl Br Me CH3 I Cl Cl Me Br CF3 Cl Br Me Br F Br Cl Et CH3 I Cl Cl Et Br CF3 Cl Br Et Br F Br Cl i-Pr CH3 I Cl Cl i-Pr Br CF3 Cl Br i-Pr Br F Br Cl t-Bu CH3 I Cl Cl t-Bu Br CF3 Cl Br t-Bu Br F Br Cl Me CH3 I Cl Br Me Br CF3 Br Cl Me Br F Br Br Et CH3 I Cl Br Et Br CF3 Br Cl Et Br F Br Br i-Pr CH3 I Cl Br i-Pr Br CF3 Br Cl i-Pr Br F Br Br t-Bu CH3 I Cl Br t-Bu Br CF3 Br Cl t-Bu Br F Br Br Me CH3 I Br Cl Me Br CF3 Br Br Me Br Cl CF3 Cl Et CH3 I Br CI Et Br CF3 Br Br Et Br Cl CF3 Cl i-Pr CH3 I Br Cl i-Pr Br CF3 Br Br i-Pr Br Cl CF3 Cl t-Bu CH3 I Br Cl t-Bu Br CF3 Br Br t-Bu Br Cl CF3 Cl Me CH3 I Br Br Me Br Br CF3 Cl Me Br Cl CF3 Br Et CH3 I Br Br Et Br Br CF3 Cl Et Br Cl CF3 Br i-Pr CH3 I Br Br i-Pr Br Br CF3 Cl i-Pr Br Cl CF3 Br t-Bu CH3 I Br Br t-Bu Br Br CF3 Cl t-Bu Br CI CF3 Br Me CH3 CF3 CF3 Cl Me Br Br CF3 Br Me Br Cl Cl Cl Et CH3 CF3 CF3 Cl Et Br Br CF3 Br Et Br Cl Cl Cl i-Pr CH3 CF3 CF3 Cl i-Pr Br Br CF3 Br i-Pr Br Cl Cl Cl t-Bu CH3 CF3 CF3 Cl t-Bu Br Br CF3 Br t-Bu Br Cl Cl Cl Me CH3 CF3 CF3 Br Me Br Br Cl Cl Me Br Cl Cl Br R3 R4a R4b R5 R6 R3 R4a R4b R5 R6 R3 R4a R4b R5 R6 Et CH3 CF3 CF3 Br Et Br Br Cl Cl Et Br Cl Cl Br i-Pr CH3 CF3 CF3 Br i-Pr Br Br Cl Cl i-Pr Br Cl Cl Br t-Bu CH3 CF3 CF3 Br t-Bu Br Br Cl Cl t-Bu Br Cl Cl Br Me CH3 CF3 Cl Cl Me Br Br Cl Br Me Br Cl Br Cl Et CH3 CF3 Cl Cl Et Br Br Cl Br Et Br Cl Br Cl i-Pr CH3 CF3 Cl Cl i-Pr Br Br Cl Br i-Pr Br Cl Br Cl t-Bu CH3 CF3 Cl Cl t-Bu Br Br Cl Br t-Bu Br Cl Br Cl Me CH3 CF3 Cl Br Me CH3 CF3 Br Cl Me Br Cl Br Br Et CH3 CF3 Cl Br Et CH3 CF3 Br Cl Et Br Cl Br Br i-Pr CH3 CF3 Cl Br i-Pr CH3 CF3 Br Cl i-Pr Br Cl Br Br t-Bu CH3 CF3 Cl Br t-Bu CH3 CF3 Br Cl t-Bu Br Cl Br Br Me CH3 CF3 Br Br n-Pr CH3 Cl Cl Cl t-Bu CH3 CF3 Br Br Et CH3 CF3 Br Br n-Bu CH3 Cl Cl Cl i-Bu CH3 Cl Cl Cl i-Pr CH3 CF3 Br Br s-Bu CH3 Cl Cl Cl Table 13 R5b is CHF2 R5b is CH2CF3 R5b is CF2CHF2 R3 R4a R4b R5a R3 R4a R4b R5a R3 R4a R4b p5a i-Pr Me H Me i-Pr Me H Me i-Pr Me H Me i-Pr Cl H Me i-Pr CI H Me i-Pr CI H Me i-Pr Me Cl Me i-Pr Me Cl Me i-Pr Me Cl Me i-Pr Cl Cl Me i-Pr Cl Cl Me i-Pr Cl Cl Me i-Pr Me Br Me i-Pr Me Br Me i-Pr Me Br Me i-Pr CI Br Me i-Pr Cl Br Me i-Pr Cl Br Me t-Bu Me H Me t-Bu Me H Me t-Bu Me H Me t-Bu Cl H Me t-Bu Cl H Me t-Bu Cl H Me t-Bu Me Cl Me t-Bu Me Cl Me t-Bu Me Cl Me t-Bu Cl Cl Me t-Bu Cl Cl Me t-Bu Cl Cl Me t-Bu Me Br Me t-Bu Me Br Me t-Bu Me Br Me t-Bu Cl Br Me t-Bu Cl Br Me t-Bu Cl Br Me R5b is CHFo R5b is CH2CF3 R5b is CF2CHF2 R3 R4a R4b R5a R3 R4a R4b R5a R3 R4a R4b R5a Et Me H Me Et Me H Me Et Me H Me Et CI H Me Et Ci H Me Et CI H Me Et Me Cl Me Et Me Cl Me Et Me Cl Me Et CI Cl Me Et Cl Cl Me Et Cl Cl Me Et Me Br Me Et Me Br Me Et Me Br Me Et Cl Br Me Et Cl Br Me Et Cl Br Me Me Me H Me Me Me H Me Me Me H Me Me Cl H Me Me Cl H Me Me Cl H Me Me Me CI Me Me Me Cl Me Me Me Cl Me Me Cl Cl Me Me Cl Cl Me Me Cl Cl Me Me Me Br Me Me Me Br Me Me Me Br Me Me Cl Br Me Me Cl Br Me Me Cl Br Me Table 14 R5b is CHF2 R5b is CH2CF3 R5b IS CF2CHF2 R3 R4a R4b R5a R3 R4a R4b R5a R3 R4a R4b R5a i-Pr Me H Me i-Pr Me H Me i-Pr Me H Me i-Pr Cl H Me i-Pr Cl H Me i-Pr Cl H Me i-Pr Me Cl Me i-Pr Me Cl Me i-Pr Me Cl Me i-Pr Cl Cl Me i-Pr Cl Cl Me i-Pr Cl Cl Me i-Pr Me Br Me i-Pr Me Br Me i-Pr Me Br Me i-Pr Cl Br Me i-Pr CI Br Me i-Pr Cl Br Me t-Bu Me H Me t-Bu Me H Me t-Bu Me H Me t-Bu Cl H Me t-Bu Cl H Me t-Bu Cl H Me t-Bu Me Cl Me t-Bu Me Cl Me t-Bu Me Cl Me t-Bu Cl Cl Me t-Bu Cl Cl Me t-Bu Cl Cl Me t-Bu Me Br Me t-Bu Me Br Me t-Bu Me Br Me t-Bu CI Br Me t-Bu Cl Br Me t-Bu Cl Br Me Et Me H Me Et Me H Me Et Me H Me Et Cl H Me Et Cl H Me Et Cl H Me R5b is CHF2 R5b is CH2CF3 R5b is CF2CHF2 R3 R4a R4b R5a R3 R4a R4b R5a R3 R4a R4b R5a Et Me CI Me Et Me Cl Me Et Me Cl Me Et Cl Cl Me Et Cl Cl Me Et Cl Cl Me Et Me Br Me Et Me Br Me Et Me Br Me Et Cl Br Me Et Cl Br Me Et Cl Br Me Me Me H Me Me Me H Me Me Me H Me Me Cl H Me Me Cl H Me Me Cl H Me Me Me Cl Me Me Me Cl Me Me Me Cl Me Me Cl Cl Me Me Cl Cl Me Me Cl Cl Me Me Me Br Me Me Me Br Me Me Me Br Me Me Cl Br Me Me Cl Br Me Me Cl Br Me Table 15 R5 is CHF2 R5 is CH2CF3 R5 is CF2CHF2 R3 R4a R4b R6 R3 R4a R4b R6 R3 R4a R4b R6 Me CH3 H Cl Me CH3 H Cl Me CH3 H Ci Et CH3 H Cl Et CH3 H Cl Et CH3 H CI i-Pr CH3 H CI i-Pr CH3 H Cl i-Pr CH3 H Cl t-Bu CH3 H Cl t-Bu CH3 H Cl t-Bu CH3 H CI Me CH3 H Br Me CH3 H Br Me CH3 H Br Et CH3 H Br Et CH3 H Br Et CH3 H Br i-Pr CH3 H Br i-Pr CH3 H Br i-Pr CH3 H Br t-Bu CH3 H Br t-Bu CH3 H Br t-Bu CH3 H Br Me CH3 F Cl Me CH3 F Cl Me CH3 F Cl Et CH3 F Cl Et CH3 F Cl Et CH3 F Cl i-Pr CH3 F Cl i-Pr CH3 F Cl i-Pr CH3 F Cl t-Bu CH3 F Cl t-Bu CH3 F Cl t-Bu CH3 F Cl Me CH3 F Br Me CH3 F Br Me CH3 F Br Et CH3 F Br Et CH3 F Br Et CH3 F Br i-Pr CH3 F Br i-Pr CH3 F Br i-Pr CH3 F Br R5 is CHF2 R5 is CH2CF3 R5 is CF2CHF2 R3 R4a R4b R6 R3 R4a R4b R6 R3 R4a R4b R6 t-Bu CH3 F Br t-Bu CH3 F Br t-Bu CH3 F Br Me CH3 Cl Cl Me CH3 Cl Cl Me CH3 Cl Cl Et CH3 Cl Cl Et CH3 Cl Cl Et CH3 Cl Cl i-Pr CH3 Cl Cl i-Pr CH3 Cl Cl i-Pr CH3 Cl Cl t-Bu CH3 Cl Cl t-Bu CH3 Cl Cl t-Bu CH3 Cl Cl Me CH3 Cl Br Me CH3 Cl Br Me CH3 Cl Br Et CH3 Cl Br Et CH3 Cl Br Et CH3 Cl Br i-Pr CH3 Cl Br i-Pr CH3 Cl Br i-Pr CH3 Cl Br t-Bu CH3 Cl Br t-Bu CH3 Cl Br t-Bu CH3 Cl Br Me CH3 Br Cl Me CH3 Br Cl Me CH3 Br Cl Et CH3 Br Cl Et CH3 Br Cl Et CH3 Br Cl i-Pr CH3 Br Cl i-Pr CH3 Br Cl i-Pr CH3 Br Cl t-Bu CH3 Br Cl t-Bu CH3 Br Cl t-Bu CH3 Br Cl Me CH3 Br Br Me CH3 Br Br Me CH3 Br Br Et CH3 Br Br Et CH3 Br Br Et CH3 Br Br i-Pr CH3 Br Br i-Pr CH3 Br Br i-Pr CH3 Br Br t-Bu CH3 Br Br t-Bu CH3 Br Br t-Bu CH3 Br Br Me CH3 I Cl Me CH3 I Cl Me CH3 I Cl Et CH3 I Cl Et CH3 I Cl Et CH3 I Cl i-Pr CH3 I Cl i-Pr CH3 I Cl i-Pr CH3 I Cl t-Bu CH3 I Cl t-Bu CH3 I Cl t-Bu CH3 I Cl Me CH3 I Br Me CH3 I Br Me CH3 I Br Et CH3 I Br Et CH3 I Br Et CH3 I Br i-Pr CH3 I Br i-Pr CH3 I Br i-Pr CH3 I Br t-Bu CH3 I Br t-Bu CH3 I Br t-Bu CH3 I Br Me CH3 CF3 Cl Me CH3 CF3 Cl Me CH3 CF3 Cl Et CH3 CF3 Cl Et CH3 CF3 Cl Et CH3 CF3 Cl i-Pr CH3 CF3 CI i-Pr CH3 CF3 Cl i-Pr CH3 CF3 Cl t-Bu CH3 CF3 Cl t-Bu CH3 CF3 Cl t-Bu CH3 CF3 Cl Me CH3 CF3 Br Me CH3 CF3 Br Me CH3 CF3 Br Et CH3 CF3 Br Et CH3 CF3 Br Et CH3 CF3 Br i-Pr CH3 CF3 Br i-Pr CH3 CF3 Br i-Pr CH3 CF3 Br t-Bu CH3 CF3 Br t-Bu CH3 CF3 Br t-Bu CH3 CF3 Br n-Pr CH3 Cl Cl Me Cl F Br Me Cl H Br n-Bu CH3 Cl Cl Et Cl F Br Et CI H Br s-Bu CH3 Cl Cl i-Pr Cl F Br i-Pr Cl H Br R5 is CHF2 R5 is CH2CF3 R5 is CF2CHF2 R3 R4a R4b R6 R3 R4a R4b R6 R3 R4a R4b R6 i-Bu CH3 Cl Cl t-Bu Cl F Br t-Bu Cl H Br Me Cl F Cl Me Cl F Cl Me Cl H Cl Et ci F ci Et Cl F ci Et ci H ci i-Pr Cl F Cl i-Pr Cl F Cl i-Pr Cl H Cl t-Bu Cl F Cl t-Bu Cl F Cl i-Pr Cl H Cl Me Cl F Br Me Cl Cl Br Me Cl I Br Et Cl F Br Et Cl Cl Br Et Cl I Br i-Pr Cl F Br i-Pr Cl Cl Br i-Pr Cl I Br t-Bu Cl F Br t-Bu Cl Cl Br t-Bu Cl I Br Me Cl Cl Cl Me Cl Cl Cl Me Cl I Cl Et Cl Cl ci Et Cl Cl Cl Et Cl I Cl i-Pr Cl Cl Cl i-Pr Cl Cl Cl i-Pr Cl I Cl t-Bu Cl Cl Cl t-Bu Cl Cl Cl t-Bu Cl I Cl Me Cl H Br Me Cl H Br Me Cl F Br Et Cl H Br Et Cl H Br Et Cl F Br i-Pr Cl H Br i-Pr Cl H Br i-Pr Cl F Br t-Bu Cl H Br t-Bu Cl H Br t-Bu Cl F Br Me Cl H Cl Me Cl H Cl Me Cl F Cl Et Cl H Cl Et Cl H Cl Et Cl F Cl i-Pr Cl H Cl i-Pr Cl H Cl i-Pr Cl F Cl t-Bu Cl H Cl t-Bu Cl H Cl t-Bu Cl F Cl Me Cl Br Br Me Cl Br Br Me Cl CF3 Br Et Cl Br Br Et Cl Br Br Et Cl CF3 Br i-Pr Cl Br Br i-Pr Cl Br Br i-Pr Cl CF3 Br t-Bu Cl Br Br t-Bu Cl Br Br t-Bu Cl CF3 Br Me Cl Br Cl Me Cl I Cl Me Cl CF3 Cl Et Cl Br Cl Et Cl I Cl Et Cl CF3 Cl i-Pr Cl Br Cl i-Pr Cl I Cl i-Pr Cl CF3 Cl t-Bu Cl Br Cl t-Bu Cl I Cl t-Bu Cl CF3 Cl Me Cl I Br Me Cl I Br Me Br F Cl Et Cl I Br Et Cl I Br Et Br F Cl i-Pr Cl I Br i-Pr Cl I Br i-Pr Br F Cl t-Bu Cl I Br t-Bu Cl I Br t-Bu Br F Cl Me Cl I Cl Me Cl CF3 Cl Me Br F Br Et Cl I Cl Et Cl CF3 Cl Et Br F Br i-Pr Cl I Cl i-Pr Cl CF3 Cl i-Pr Br F Br R5 is CHF2 R5 is CH2CF3 R% is CF2CHF2 R3 R4a R4b R6 R3 R4a R4b R6 R3 R4a R4b R6 t-Bu Cl I Cl t-Bu Cl CF3 Cl t-Bu Br F Br Me Cl CF3 Br Me Cl CF3 Br Me Br Cl Cl Et Cl CF3 Br Et Cl CF3 Br Et Br Cl Cl i-Pr Cl CF3 Br i-Pr Cl CF3 Br i-Pr Br Cl Cl t-Bu Cl CF3 Br t-Bu Cl CF3 Br t-Bu Br Cl Cl Me Cl CF3 Cl n-Pr Cl Cl Cl Me Br Cl Br Et Cl CF3 Cl n-Bu Cl Cl Cl Et Br Cl Br i-Pr Cl CF3 Cl s-Bu Cl Cl Cl i-Pr Br Cl Br t-Bu Cl CF3 Cl i-Bu Cl Cl Cl t-Bu Br Cl Br Me Br F Cl Me Br F Cl Me Br Br Cl Et Br F CI Et Br F CI Et Br Br ci i-Pr Br F Cl i-Pr Br F Cl i-Pr Br Br Cl t-Bu Br F Cl t-Bu Br F Cl t-Bu Br Br Cl Me Br F Br Me Br F Br Me Br Br Br Et Br F Br Et Br F Br Et Br Br Br i-Pr Br F Br i-Pr Br F Br i-Pr Br Br Br t-Bu Br F Br t-Bu Br F Br t-Bu Br Br Br Me Br Cl Cl Me Br CI Cl Me Br I Cl Et Br CI Cl Et Br Cl Cl Et Br I Cl i-Pr Br Cl Cl i-Pr Br Cl CI i-Pr Br I Cl t-Bu Br Cl Cl t-Bu Br Cl Cl t-Bu Br I Cl Me Br Cl Br Me Br CI Br Me Br I Br Et Br Cl Br Et Br CI Br Et Br I Br i-Pr Br Cl Br i-Pr Br Cl Br i-Pr Br I Br t-Bu Br Cl Br t-Bu Br Cl Br t-Bu Br I Br Me Br Br Cl Me Br Br Cl Me Br CF3 Cl Et Br Br Cl Et Br Br Cl Et Br CF3 Cl i-Pr Br Br CI i-Pr Br Br Cl i-Pr Br CF3 Cl t-Bu Br Br Cl t-Bu Br Br Cl t-Bu Br CF3 Cl Me Br Br Br Me Br Br Br Me Br CF3 Br Et Br Br Br Et Br Br Br Et Br CF3 Br i-Pr Br Br Br i-Pr Br Br Br i-Pr Br CF3 Br t-Bu Br Br Br t-Bu Br Br Br t-Bu Br CF3 Br Me Br I CI Me Br I Cl Me Cl Cl Br Et Br I Cl Et Br I Cl Et Cl Cl Br i-Pr Br I Cl i-Pr Br I Cl i-Pr Cl Cl Br R5 is CHF2 R5 is CH2CF3 R5 is CF2CHF2 R3 R4a R4b R6 R3 R4a R4b R6 R3 R4a R4b R6 t-Bu Br I CI t-Bu Br I Cl t-Bu Cl Cl Br Me Br I Br Me Br I Br Me Cl Cl Cl Et Br I Br Et Br I Br Et Cl Cl cl i-Pr Br I Br i-Pr Br I Br i-Pr Cl Cl Cl t-Bu Br I Br t-Bu Br I Br t-Bu Cl Cl Cl Table 16 R5 is CHF2 R5 is CH2CF3 R5 is cF2CHF2 R3 R4a R4b R6 R3 R4a R4b R6 R3 R4a R4b R6 Me CH3 H Cl Me CH3 H Cl Me CH3 H Cl Et CH3 H Cl Et CH3 H Cl Et CH3 H Cl i-Pr CH3 H Cl i-Pr CH3 H Cl i-Pr CH3 H Cl t-Bu CH3 H Cl t-Bu CH3 H Cl t-Bu CH3 H Cl Me CH3 H Br Me CH3 H Br Me CH3 H Br Et CH3 H Br Et CH3 H Br Et CH3 H Br i-Pr CH3 H Br i-Pr CH3 H Br i-Pr CH3 H Br t-Bu CH3 H Br t-Bu CH3 H Br t-Bu CH3 H Br Me CH3 F Cl Me CH3 F Cl Me CH3 F Cl Et CH3 F Cl Et CH3 F Cl Et CH3 F Cl i-Pr CH3 F Cl i-Pr CH3 F Cl i-Pr CH3 F Cl t-Bu CH3 F Cl t-Bu CH3 F Cl t-Bu CH3 F Cl Me CH3 F Br Me CH3 F Br Me CH3 F Br Et CH3 F Br Et CH3 F Br Et CH3 F Br i-Pr CH3 F Br i-Pr CH3 F Br i-Pr CH3 F Br t-Bu CH3 F Br t-Bu CH3 F Br t-Bu CH3 F Br Me CH3 Cl Cl Me CH3 Cl Cl Me CH3 Cl Cl Et CH3 Cl Cl Et CH3 Cl Cl Et CH3 Cl Cl i-Pr CH3 Cl Cl i-Pr CH3 Cl Cl i-Pr CH3 Cl CI t-Bu CH3 Cl Cl t-Bu CH3 Cl Cl t-Bu CH3 Cl Cl Me CH3 Cl Br Me CH3 Cl Br Me CH3 Cl Br R5 is CHF2 R5 is CH2CF3 R5 is CF2CHF2 R3 R4a R4b R6 R3 R4a R4b R6 R3 R4a R4b R6 Et CH3 Cl Br Et CH3 Cl Br Et CH3 Cl Br i-Pr CH3 Cl Br i-Pr CH3 Cl Br i-Pr CH3 CI Br t-Bu CH3 Cl Br t-Bu CH3 Cl Br t-Bu CH3 Cl Br Me CH3 Br Cl Me CH3 Br Cl Me CH3 Br Cl Et CH3 Br Cl Et CH3 Br Cl Et CH3 Br Cl i-Pr CH3 Br Cl i-Pr CH3 Br Cl i-Pr CH3 Br Cl t-Bu CH3 Br CI t-Bu CH3 Br Cl t-Bu CH3 Br Cl Me CH3 Br Br Me CH3 Br Br Me CH3 Br Br Et CH3 Br Br Et CH3 Br Br Et CH3 Br Br i-Pr CH3 Br Br i-Pr CH3 Br Br i-Pr CH3 Br Br t-Bu CH3 Br Br t-Bu CH3 Br Br t-Bu CH3 Br Br Me CH3 I Cl Me CH3 I Cl Me CH3 I Cl Et CH3 I Cl Et CH3 I CI Et CH3 I Cl i-Pr CH3 I Cl i-Pr CH3 I Cl i-Pr CH3 I Cl t-Bu CH3 I Cl t-Bu CH3 I Cl t-Bu CH3 I Cl Me CH3 I Br Me CH3 I Br Me CH3 I Br Et CH3 I Br Et CH3 I Br Et CH3 I Br i-Pr CH3 I Br i-Pr CH3 I Br i-Pr CH3 I Br t-Bu CH3 I Br t-Bu CH3 I Br t-Bu CH3 I Br Me CH3 CF3 Cl Me CH3 CF3 Cl Me CH3 CF3 CI Et CH3 CF3 Cl Et CH3 CF3 Cl Et CH3 CF3 Cl i-Pr CH3 CF3 Cl i-Pr CH3 CF3 Cl i-Pr CH3 CF3 Cl t-Bu CH3 CF3 Cl t-Bu CH3 CF3 Cl t-Bu CH3 CF3 Cl Me CH3 CF3 Br Me CH3 CF3 Br Me CH3 CF3 Br Et CH3 CF3 Br Et CH3 CF3, Br Et CH3 CF3 Br i-Pr CH3 CF3 Br i-Pr CH3 CF3 Br i-Pr CH3 CF3 Br t-Bu CH3 CF3 Br t-Bu CH3 CF3 Br t-Bu CH3 CF3 Br n-Pr CH3 Cl Cl Me Cl F Br Me Cl H Br n-Bu CH3 CI Cl Et Cl F Br Et Cl H Br s-Bu CH3 Cl Cl i-Pr Cl F Br i-Pr Cl H Br i-Bu CH3 Cl Cl t-Bu Cl F Br t-Bu Cl H Br Me Cl F Cl Me Cl F Cl Me Cl H Cl Et Cl F Cl Et ci F ci Et Cl H ci i-Pr Cl F Cl i-Pr Cl F Cl i-Pr CI H Cl t-Bu Cl F CI t-Bu Cl F Cl i-Pr Cl H Cl Me Cl F Br Me Cl Cl Br Me Cl I Br R5 is CHF2 R5 is CH2CF3 R5 is CF2CHF2 R3 R4a R4b R6 R3 R4a R4b R6 R3 R4a R4b R6 Et Ci F Br Et Cl Cl Br Et Cl I Br i-Pr Cl F Br i-Pr Cl Cl Br i-Pr Cl I Br t-Bu Cl F Br t-Bu Cl Cl Br t-Bu Cl I Br Me Cl Cl Cl Me Cl CI Cl Me Cl I Cl Et Cl Cl Cl Et Cl Cl Cl Et Cl I Cl i-Pr Cl Cl Cl i-Pr CI Cl Cl i-Pr Cl I Cl t-Bu Cl Cl Cl t-Bu Cl Cl Cl t-Bu Cl I Cl Me Cl H Br Me Cl H Br Me CI F Br Et Cl H Br Et CI H Br Et Cl F Br i-Pr Cl H Br i-Pr Cl H Br i-Pr Cl F Br t-Bu Cl H Br t-Bu Cl H Br t-Bu Cl F Br Me CI H Cl Me Cl H Cl Me Cl F Cl Et CI H Cl Et Cl H Cl Et Cl F Cl i-Pr Cl H Cl i-Pr Cl H CI i-Pr Cl F CI t-Bu Cl H Cl t-Bu Cl H Cl t-Bu Cl F Cl Me CI Br Br Me Cl Br Br Me Cl CF3 Br Et Cl Br Br Et Cl Br Br Et Cl CF3 Br i-Pr Cl Br Br i-Pr Cl Br Br i-Pr Cl CF3 Br t-Bu Cl Br Br t-Bu Cl Br Br t-Bu Cl CF3 Br Me Cl Br Cl Me Cl I CI Me Cl CF3 Cl Et Cl Br CI Et Cl I Cl Et Cl CF3 Cl i-Pr Cl Br Cl i-Pr Cl I Cl i-Pr Cl CF3 Cl t-Bu Cl Br Cl t-Bu Cl I Cl t-Bu Cl CF3 Cl Me Cl I Br Me Cl I Br Me Br F Cl Et Cl I Br Et CI I Br Et Br F CI i-Pr Cl I Br i-Pr Cl I Br i-Pr Br F Cl t-Bu Cl I Br t-Bu Cl I Br t-Bu Br F Cl Me Cl I Cl Me Cl CF3 Cl Me Br F Br Et CI I Cl Et Cl CF3 Cl Et Br F Br i-Pr Cl I Cl i-Pr Cl CF3 Cl i-Pr Br F Br t-Bu Cl I Cl t-Bu Cl CF3 Cl t-Bu Br F Br Me Cl CF3 Br Me Cl CF3 Br Me Br Cl Cl Et Cl CF3 Br Et Cl CF3 Br Et Br Cl Cl i-Pr Cl CF3 Br i-Pr Cl CF3 Br i-Pr Br Cl Cl t-Bu Cl CF3 Br t-Bu Cl CF3 Br t-Bu Br CI Cl Me CI CF3 Cl n-Pr Cl Cl Cl Me Br Cl Br RS is CHFO RS is CH2CF3 R5 is CF2CHF2 R3 R4a R4b R6 R3 R4a R4b R6 R3 R4a R4b R6 Et Cl CF3 Cl n-Bu Cl Cl Cl Et Br Cl Br i-Pr Cl CF3 Cl s-Bu Cl Cl Cl i-Pr Br Cl Br t-Bu Cl CF3 Cl i-Bu Cl Cl Cl t-Bu Br Cl Br Me Br F Cl Me Br F CI Me Br Br Cl Et Br F CI Et Br F Cl Et Br Br Ci i-Pr Br F Cl i-Pr Br F Cl i-Pr Br Br Cl t-Bu Br F Cl t-Bu Br F Cl t-Bu Br Br Cl Me Br F Br Me Br F Br Me Br Br Br Et Br F Br Et Br F Br Et Br Br Br i-Pr Br F Br i-Pr Br F Br i-Pr Br Br Br t-Bu Br F Br t-Bu Br F Br t-Bu Br Br Br Me Br Cl Cl Me Br Cl Cl Me Br I Cl Et Br Cl Cl Et Br Cl Cl Et Br I Cl i-Pr Br Cl Cl i-Pr Br Cl Cl i-Pr Br I Cl t-Bu Br Cl Cl t-Bu Br Cl Cl t-Bu Br I Cl Me Br Cl Br Me Br Cl Br Me Br I Br Et Br Cl Br Et Br Cl Br Et Br I Br i-Pr Br CI Br i-Pr Br Cl Br i-Pr Br I Br t-Bu Br Cl Br t-Bu Br Cl Br t-Bu Br I Br Me Br Br Cl Me Br Br Cl Me Br CF3 Cl Et Br Br Cl Et Br Br Cl Et Br CF3 Cl i-Pr Br Br Cl i-Pr Br Br Cl i-Pr Br CF3 Cl t-Bu Br Br Cl t-Bu Br Br Cl t-Bu Br CF3 Cl Me Br Br Br Me Br Br Br Me Br CF3 Br Et Br Br Br Et Br Br Br Et Br CF3 Br i-Pr Br Br Br i-Pr Br Br Br i-Pr Br CF3 Br t-Bu Br Br Br t-Bu Br Br Br t-Bu Br CF3 Br Me Br I Cl Me Br I Cl Me Cl Cl Br Et Br I Cl Et Br I Cl Et Cl Cl Br i-Pr Br I Cl i-Pr Br I Cl i-Pr Cl Cl Br t-Bu Br I Cl t-Bu Br I Cl t-Bu Cl Cl Br Me Br I Br Me Br I Br Me Cl Cl Cl Et Br I Br Et Br I Br Et Cl Cl Cl i-Pr Br I Br i-Pr Br I Br i-Pr Cl Cl Cl t-Bu Br I Br t-Bu Br I Br t-Bu Cl Cl Cl Table 17 R5 is CH R5 is CH2E3 R5 is CF2CHF2 R3 R4a R4b R6 R3 R4a R4b R6 R3 R4a R4b R6 Me CH3 H Cl Me CH3 H Cl Me CH3 Br Cl Et CH3 H Cl Et CH3 H Cl Et CH3 Br Cl i-Pr CH3 H Cl i-Pr CH3 H Cl i-Pr CH3 Br Cl t-Bu CH3 H Cl t-Bu CH3 H Cl t-Bu CH3 Br Cl Me CH3 H Br Me CH3 H Br Me CH3 Br Br Et CH3 H Br Et CH3 H Br Et CH3 Br Br i-Pr CH3 H Br i-Pr CH3 H Br i-Pr CH3 Br Br t-Bu CH3 H Br t-Bu CH3 H Br t-Bu CH3 Br Br Me CH3 F Cl Me CH3 Br Cl Me CH3 I Cl Et CH3 F Cl Et CH3 Br Cl Et CH3 I Cl i-Pr CH3 F Cl i-Pr CH3 Br Cl i-Pr CH3 I Cl t-Bu CH3 F CI t-Bu CH3 Br Cl t-Bu CH3 I Cl Me CH3 F Br Me CH3 Br Br Me CH3 I Br Et CH3 F Br Et CH3 Br Br Et CH3 I Br i-Pr CH3 F Br i-Pr CH3 Br Br i-Pr CH3 I Br t-Bu CH3 F Br t-Bu CH3 Br Br t-Bu CH3 I Br Me CH3 Cl Cl Me CH3 F Cl Me CH3 CF3 Cl Et CH3 Cl Cl Et CH3 F Cl Et CH3 CF3 Cl i-Pr CH3 CI Cl i-Pr CH3 F Cl i-Pr CH3 CF3 CI t-Bu CH3 Cl Cl t-Bu CH3 F Cl t-Bu CH3 CF3 Cl Me CH3 Cl Br Me CH3 F Br Me CH3 CF3 Br Et CH3 Cl Br Et CH3 F Br Et CH3 CF3 Br i-Pr CH3 CI Br i-Pr CH3 F Br i-Pr CH3 CF3 Br t-Bu CH3 Cl Br t-Bu CH3 F Br t-Bu CH3 CF3 Br Me CH3 Br Cl Me CH3 Cl Cl Me CH3 Cl Cl Et CH3 Br CI Et CH3 Cl Cl Et CH3 Cl Cl i-Pr CH3 Br Cl i-Pr CH3 Cl Cl i-Pr CH3 Cl Cl t-Bu CH3 Br Cl t-Bu CH3 Cl CI t-Bu CH3 Cl CI R5 is CHF2 R5 is CH2F3 R5 is CF2CHF2 R3 R4a R4b R6 R3 R4a R4b R6 R3 R4a R4b R6 Me CH3 Br Br Me CH3 Cl Br Me CH3 Cl Br Et CH3 Br Br Et CH3 Cl Br Et CH3 Cl Br i-Pr CH3 Br Br i-Pr CH3 Cl Br i-Pr CH3 Cl Br t-Bu CH3 Br Br t-Bu CH3 Cl Br t-Bu CH3 Cl Br Me CH3 I Cl Me CH3 I Cl Me CH3 H Cl Et CH3 I Cl Et CH3 I Cl Et CH3 H Cl i-Pr CH3 I Cl i-Pr CH3 I Cl i-Pr CH3 H CI t-Bu CH3 I Cl t-Bu CH3 I Cl t-Bu CH3 H Cl Me CH3 I Br Me CH3 I Br Me CH3 H Br Et CH3 I Br Et CH3 I Br Et CH3 H Br i-Pr CH3 I Br i-Pr CH3 I Br i-Pr CH3 H Br t-Bu CH3 I Br t-Bu CH3 I Br t-Bu CH3 H Br Me CH3 CF3 CI Me CH3 CF3 Cl Me CH3 F Cl Et CH3 CF3 Cl Et CH3 CF3 Cl Et CH3 F Cl i-Pr CH3 CF3 Cl i-Pr CH3 CF3 Cl i-Pr CH3 F Cl t-Bu CH3 CF3 Cl t-Bu CH3 CF3 Cl t-Bu CH3 F Cl Me CH3 CF3 Br Me CH3 CF3 Br Me CH3 F Br Et CH3 CF3 Br Et CH3 CF3 Br Et CH3 F Br i-Pr CH3 CF3 Br i-Pr CH3 CF3 Br i-Pr CH3 F Br t-Bu CH3 CF3 Br t-Bu CH3 CF3 Br t-Bu CH3 F Br n-Pr CH3 Cl Cl Me Cl H Br Me Cl Cl Br n-Bu CH3 Cl Cl Et Cl H Br Et Cl Cl Br s-Bu CH3 Cl Cl i-Pr Cl H Br i-Pr Cl Cl Br i-Bu CH3 Cl Cl t-Bu Cl H Br t-Bu Cl Cl Br Me Cl I Br Me Cl H Cl Me Cl Cl Cl Et Cl I Br Et Cl H Cl Et Cl Cl Cl i-Pr Cl I Br i-Pr Cl H Cl i-Pr Cl Cl Cl t-Bu Cl I Br t-Bu Cl H Cl t-Bu CI Cl Cl Me Cl I Cl Me Cl Cl Br Me Cl I Br Et CI I ci Et Cl Cl Br Et CI I Br i-Pr Cl I Cl i-Pr Cl Cl Br i-Pr Cl I Br t-Bu Cl I Cl t-Bu Cl Cl Br t-Bu Cl I Br Me Cl H Br Me Cl Cl Cl Me Cl I Cl Et Cl H Br Et Cl Cl Cl Et Cl I Cl i-Pr Cl H Br i-Pr Cl Cl Cl i-Pr Cl I Cl t-Bu Cl H Br t-Bu Cl Cl Cl t-Bu Cl I Cl R5 is CHF2 R5 is CH2F3 R5 is CF2CHF2 R3 R4a R4b R6 R3 R4a R4b R6 R3 R4a R4b R6 Me Cl H Cl Me CI F Br Me Cl F Br Et Cl H Cl Et Cl F Br Et Cl F Br i-Pr Cl H Cl i-Pr Cl F Br i-Pr Cl F Br t-Bu Cl H Cl t-Bu Cl F Br t-Bu Cl F Br Me Cl CF3 Br Me Cl F Cl Me Cl F Cl Et Cl CF3 Br Et Cl F Cl Et CI F Cl i-Pr Cl CF3 Br i-Pr Cl F Cl i-Pr Cl F Cl t-Bu Cl CF3 Br t-Bu Cl F Cl t-Bu Cl F Cl Me Cl CF3 Cl Me Cl Br Br Me Cl H Br Et CI CF3 Cl Et Cl Br Br Et Cl H Br i-Pr Cl CF3 Cl i-Pr Cl Br Br i-Pr Cl H Br t-Bu Cl CF3 Cl t-Bu Cl Br Br t-Bu Cl H Br Me Cl Br Br Me Cl I Cl Me Cl H Cl Et Cl Br Br Et Cl I Cl Et Cl H Cl i-Pr Cl Br Br i-Pr Cl I Cl i-Pr Cl H Cl t-Bu Cl Br Br t-Bu CI I Cl i-Pr Cl H Cl Me Cl Br Cl Me Cl I Br Me Cl CF3 Br Et Cl Br Cl Et Cl I Br Et Cl CF3 Br i-Pr Cl Br Cl i-Pr Cl I Br i-Pr Cl CF3 Br t-Bu Cl Br Cl t-Bu Cl I Br t-Bu Cl CF3 Br Me Cl F Br Me Cl CF3 Cl Me Cl CF3 Cl Et Cl F Br Et Cl CF3 Cl Et Cl CF3 Cl i-Pr Cl F Br i-Pr ClCF3 Cl i-Pr Cl CF3 Cl t-Bu Cl F Br t-Bu Cl CF3 Cl t-Bu Cl CF3 Cl Me Cl Cl Cl Me Cl CF3 Br Me Br F Cl Et Cl Cl Cl Et CI CF3 Br Et Br F Cl i-Pr Cl Cl Cl i-Pr Cl CF3 Br i-Pr Br F Cl t-Bu Cl Cl Cl t-Bu Cl CF3 Br t-Bu Br F Cl Me Cl F Cl n-Pr Cl Cl Cl Me Br F Br Et Cl F Cl n-Bu Cl Cl Cl Et Br F Br i-Pr Cl F Cl s-Bu Cl Cl Cl i-Pr Br F Br t-Bu Cl F Cl i-Bu Cl Cl Cl t-Bu Br F Br Me Br Br CI Me Br F Cl Me Br Cl Cl Et Br Br Cl Et Br F Cl Et Br Cl Cl i-Pr Br Br Cl i-Pr Br F Cl i-Pr Br Cl Cl t-Bu Br Br Cl t-Bu Br F Cl t-Bu Br Cl Cl R5 is CHF2 R5 is CH2F3 RS is CF2CHF2 R3 R4a R4b R6 R3 R4a R4b R6 R3 R4a R4b R6 Me Br Br Br Me Br F Br Me Br Cl Br Et Br Br Br Et Br F Br Et Br Cl Br i-Pr Br Br Br i-Pr Br F Br i-Pr Br Cl Br t-Bu Br Br Br t-Bu Br F Br t-Bu Br Cl Br Me Br I Cl Me Br Cl Cl Me Br Br Cl Et Br I Cl Et Br Cl Cl Et Br Br Cl i-Pr Br I Cl i-Pr Br Cl Cl i-Pr Br Br CI t-Bu Br I Cl t-Bu Br Cl Cl t-Bu Br Br Cl Me Br I Br Me Br Cl Br Me Br Br Br Et Br I Br Et Br Cl Br Et Br Br Br i-Pr Br I Br i-Pr Br Cl Br i-Pr Br Br Br t-Bu Br I Br t-Bu Br Cl Br t-Bu Br Br Br Me Br F Cl Me Br I Cl Me Br CF3 Cl Et Br F Cl Et Br I Cl Et Br CF3 Cl i-Pr Br F Cl i-Pr Br I Cl i-Pr Br CF3 Cl t-Bu Br F Cl t-Bu Br I Cl t-Bu Br CF3 Cl Me Br F Br Me Br I Br Me Br CF3 Br Et Br F Br Et Br I Br Et Br CF3 Br i-Pr Br F Br i-Pr Br I Br i-Pr Br CF3 Br t-Bu Br F Br t-Bu Br I Br t-Bu Br CF3 Br Me Br CI Cl Me Br Br Cl Me Br I Cl Et Br Cl Cl Et Br Br Cl Et Br I Cl i-Pr Br Cl Cl i-Pr Br Br CI i-Pr Br I CI t-Bu Br Cl Cl t-Bu Br Br Cl t-Bu Br I Cl Me Br Cl Br Me Br Br Br Me Br I Br Et Br Cl Br Et Br Br Br Et Br I Br i-Pr Br Cl Br i-Pr Br Br Br i-Pr Br I Br t-Bu Br Cl Br t-Bu Br Br Br t-Bu Br I Br Table 1 S R5 is CHF2 R5 is CH2F3 R5 is CF2CHF2 R3 R4a R4b R6 R3 R4a R4b R6 R3 R4a R4b R6 Me CH3 H Cl Me CH3 H Cl Me CH3 Br Cl Et CH3 H Cl Et CH3 H Cl Et CH3 Br Cl i-Pr CH3 H Cl i-Pr CH3 H Cl i-Pr CH3 Br Cl t-Bu CH3 H Cl t-Bu CH3 H Cl t-Bu CH3 Br Cl Me CH3 H Br Me CH3 H Br Me CH3 Br Br Et CH3 H Br Et CH3 H Br Et CH3 Br Br i-Pr CH3 H Br i-Pr CH3 H Br i-Pr CH3 Br Br t-Bu CH3 H Br t-Bu CH3 H Br t-Bu CH3 Br Br Me CH3 F Cl Me CH3 Br Cl Me CH3 I Cl Et CH3 F Cl Et CH3 Br Cl Et CH3 I Cl i-Pr CH3 F Cl i-Pr CH3 Br Cl i-Pr CH3 I Cl t-Bu CH3 F Cl t-Bu CH3 Br CI t-Bu CH3 I Cl Me CH3 F Br Me CH3 Br Br Me CH3 I Br Et CH3 F Br Et CH3 Br Br Et CH3 I Br i-Pr CH3 F Br i-Pr CH3 Br Br i-Pr CH3 I Br t-Bu CH3 F Br t-Bu CH3 Br Br t-Bu CH3 I Br Me CH3 Cl Cl Me CH3 F Cl Me CH3 CF3 Cl Et CH3 Cl Cl Et CH3 F Cl Et CH3 CF3 Cl i-Pr CH3 CI Cl i-Pr CH3 F Cl i-Pr CH3 CF3 CI t-Bu CH3 Cl Cl t-Bu CH3 F Cl t-Bu CH3 CF3 Cl Me CH3 Cl Br Me CH3 F Br Me CH3 CF3 Br Et CH3 Cl Br Et CH3 F Br Et CH3 CF3 Br i-Pr CH3 Cl Br i-Pr CH3 F Br i-Pr CH3 CF3 Br t-Bu CH3 Cl Br t-Bu CH3 F Br t-Bu CH3 CF3 Br Me CH3 Br Cl Me CH3 Cl Cl Me CH3 Cl Cl Et CH3 Br Cl Et CH3 Cl CI Et CH3 Cl Cl i-Pr CH3 Br Cl i-Pr CH3 Cl Cl i-Pr CH3 Cl Cl t-Bu CH3 Br Cl t-Bu CH3 Cl Cl t-Bu CH3 Cl Cl Me CH3 Br Br Me CH3 Cl Br Me CH3 Cl Br R5 is cHF2 R5 is CH2F3 R5 is CF2CHF2 R3 R4a R4b R6 R3 R4a R4b R6 R3 R4a R4b R6 Et CH3 Br Br Et CH3 Cl Br Et CH3 Cl Br i-Pr CH3 Br Br i-Pr CH3 Cl Br i-Pr CH3 Cl Br t-Bu CH3 Br Br t-Bu CH3 Cl Br t-Bu CH3 Cl Br Me CH3 I Cl Me CH3 I Cl Me CH3 H Cl Et CH3 I Cl Et CH3 I Cl Et CH3 H Cl i-Pr CH3 I Cl i-Pr CH3 I Cl i-Pr CH3 H Cl t-Bu CH3 I Cl t-Bu CH3 I Cl t-Bu CH3 H Cl Me CH3 I Br Me CH3 I Br Me CH3 H Br Et CH3 I Br Et CH3 I Br Et CH3 H Br i-Pr CH3 I Br i-Pr CH3 I Br i-Pr CH3 H Br t-Bu CH3 I Br t-Bu CH3 I Br t-Bu CH3 H Br Me CH3 CF3 CI Me CH3 CF3 CI Me CH3 F Cl Et CH3 CF3 Cl Et CH3 CF3 Cl Et CH3 F Cl i-Pr CH3 CF3 Cl i-Pr CH3 CF3 Cl i-Pr CH3 F Cl t-Bu CH3 CF3 Cl t-Bu CH3 CF3 Cl t-Bu CH3 F Cl Me CH3 CF3 Br Me CH3 CF3 Br Me CH3 F Br Et CH3 CF3 Br Et CH3 CF3 Br Et CH3 F Br i-Pr CH3 CF3 Br i-Pr CH3 CF3 Br i-Pr CH3 F Br t-Bu CH3 CF3 Br t-Bu CH3 CF3 Br t-Bu CH3 F Br n-Pr CH3 Cl Cl Me Cl H Br Me Cl Cl Br M-Bu CH3 Cl Cl Et Cl H Br Et Cl Cl Br s-Bu CH3 Cl Cl i-Pr Cl H Br i-Pr Cl Cl Br i-Bu CH3 Cl Cl t-Bu Cl H Br t-Bu Cl Cl Br Me Cl I Br Me Cl H Cl Me Cl Cl Cl Et Cl I Br Et Cl H Cl Et Cl CI Cl i-Pr CI I Br i-Pr Cl H Cl i-Pr Cl Cl Cl t-Bu Cl I Br t-Bu Cl H Cl t-Bu Cl Cl Cl Me Cl I Cl Me Cl Cl Br Me Cl I Br Et CI I cl Et ci Cl Br Et Cl I Br i-Pr Cl I Cl i-Pr Cl Cl Br i-Pr Cl I Br t-Bu Cl I Cl t-Bu Cl Cl Br t-Bu CI I Br Me Cl H Br Me Cl Cl Cl Me Cl I Cl Et ci H Br Et Cl Cl Cl Et Cl I Cl i-Pr CI H Br i-Pr Cl CI Cl i-Pr Cl I Cl t-Bu Cl H Br t-Bu Cl Cl Cl t-Bu CI I Cl Me Cl H Cl Me Cl F Br Me Cl F Br R5 is CHF2 R5 is CH2F3 R5 is CF2CHF2 R3 R4a R4b R6 R3 R4a R4b R6 R3 R4a R4b R6 Et ci H Cl Et Cl F Br Et Cl F Br i-Pr Cl H Cl i-Pr Cl F Br i-Pr Cl F Br t-Bu Cl H Cl t-Bu Cl F Br t-Bu Cl F Br Me Cl CF3 Br Me Cl F Cl Me Cl F Cl Et Cl CF3 Br Et ci F ci Et Cl F Cl i-Pr Cl CF3 Br i-Pr Cl F Cl i-Pr Cl F Cl t-Bu Cl CF3 Br t-Bu Cl F Cl t-Bu Cl F Cl Me Cl CF3 Cl Me Cl Br Br Me Cl H Br Et Cl CF3 Cl Et Cl Br Br Et Cl H Br i-Pr Cl CF3 Cl i-Pr Cl Br Br i-Pr Cl H Br t-Bu Cl CF3 Cl t-Bu Cl Br Br t-Bu Cl H Br Me Cl Br Br Me Cl I Cl Me Cl H Cl Et Cl Br Br Et Cl I ci Et Cl H ci i-Pr Cl Br Br i-Pr Cl I Cl i-Pr Cl H Cl t-Bu Cl Br Br t-Bu Cl I Cl i-Pr Cl H Cl Me Cl Br Cl Me Cl I Br Me Cl CF3 Br Et Cl Br Cl Et Cl I Br Et Cl CF3 Br i-Pr Cl Br Cl i-Pr Cl I Br i-Pr Cl CF3 Br t-Bu Cl Br Cl t-Bu Cl I Br t-Bu Cl CF3 Br Me Cl F Br Me Cl CF3 Cl Me Cl CF3 Cl Et Cl F Br Et Cl CF3 Cl Et Cl CF3 Cl i-Pr Cl F Br i-Pr Cl CF3 Cl i-Pr Cl CF3 Cl t-Bu Cl F Br t-Bu Cl CF3 Cl t-Bu Cl CF3 Cl Me Cl Cl Cl Me Cl CF3 Br Me Br F Cl Et Cl ci Cl Et Cl CF3 Br Et Br F ci i-Pr Cl Cl Cl i-Pr Cl CF3 Br i-Pr Br F Cl t-Bu Cl Cl Cl t-Bu Cl CF3 Br t-Bu Br F Cl Me Cl F Cl n-Fr Cl Cl Cl Me Br F Br Et Cl F Cl n-Bu Cl Cl Cl Et Br F Br i-Pr Cl F Cl s-Bu Cl Cl Cl i-Pr Br F Br t-Bu Cl F Cl i-Bu Cl Cl Cl t-Bu Br F Br Me Br Br Cl Me Br F Cl Me Br Cl Cl Et Br Br Cl Et Br F ci Et Br Cl Cl i-Pr Br Br Cl i-Pr Br F Cl i-Pr Br Cl Cl t-Bu Br Br Cl t-Bu Br F Cl t-Bu Br Cl Cl Me Br Br Br Me Br F Br Me Br Cl Br R5 is CHF2 R5 is CHIEZ R5 is CH2CHF2 R3 R4a R4b R6 R3 R4a R4b R6 R3 R4a R4b R6 Et Br Br Br Et Br F Br Et Br Cl Br i-Pr Br Br Br i-Pr Br F Br i-Pr Br Cl Br t-Bu Br Br Br t-Bu Br F Br t-Bu Br Cl Br Me Br I Cl Me Br Cl Cl Me Br Br Cl Et Br I Cl Et Br CI CI Et Br Br CI i-Pr Br I Cl i-Pr Br Cl Cl i-Pr Br Br Cl t-Bu Br I Cl t-Bu Br CI Cl t-Bu Br Br Cl Me Br I Br Me Br Cl Br Me Br Br Br Et Br I Br Et Br Cl Br Et Br Br Br i-Pr Br I Br i-Pr Br CI Br i-Pr Br Br Br t-Bu Br I Br t-Bu Br CI Br t-Bu Br Br Br Me Br F Cl Me Br I Cl Me Br CF3 Cl Et Br F ci Et Br I Cl Et Br CF3 CI i-Pr Br F Cl i-Pr Br I Cl i-Pr Br CF3 Cl t-Bu Br F Cl t-Bu Br I Cl t-Bu Br CF3 Cl Me Br F Br Me Br I Br Me Br CF3 Br Et Br F Br Et Br I Br Et Br CF3 Br i-Pr Br F Br i-Pr Br I Br i-Pr Br CF3 Br t-Bu Br F Br t-Bu Br I Br t-Bu Br CF3 Br Me Br Cl Cl Me Br Br Cl Me Br I Cl Et Br Cl Cl Et Br Br Cl Et Br I ci i-Pr Br Cl Cl i-Pr Br Br Cl i-Pr Br I Cl t-Bu Br Cl Cl t-Bu Br Br Cl t-Bu Br I Cl Me Br Cl Br Me Br Br Br Me Br I Br Et Br Cl Br Et Br Br Br Et Br I Br i-Pr Br Cl Br i-Pr Br Br Br i-Pr Br I Br t-Bu Br Cl Br t-Bu Br Br Br t-Bu Br I Br Table 19 R5b is Cl R5b is CF3 R5b is OCF3 R5b is CF(CH3)2 R3 R4a R4b R3 R4a R4b R3 R4a R4b R3 R4a R4b i-Pr Me H i-Pr Me H i-Pr Me H i-Pr Me H i-Pr Cl H i-Pr Cl H i-Pr Cl H i-Pr Cl H i-Pr Me Cl i-Pr Me Cl i-Pr Me CI i-Pr Me Cl i-Pr Cl Cl i-Pr Cl Cl i-Pr Cl Cl i-Pr Cl Cl i-Pr Me Br i-Pr Me Br i-Pr Me Br i-Pr Me Br i-Pr Cl Br i-Pr Cl Br i-Pr Cl Br i-Pr Cl Br t-Bu Me H t-Bu Me H t-Bu Me H t-Bu Me H t-Bu Cl H t-Bu Cl H t-Bu Cl H t-Bu Cl H t-Bu Me Cl t-Bu Me Cl t-Bu Me CI t-Bu Me Cl t-Bu Cl Cl t-Bu Cl Cl t-Bu Cl Cl t-Bu Cl Cl t-Bu Me Br t-Bu Me Br t-Bu Me Br t-Bu Me Br t-Bu Cl Br t-Bu Cl Br t-Bu Cl Br t-Bu Cl Br Et Me H Et Me H Et Me H Et Me H Et ci H Et ci H Et ci H Et Cl H Et Me Cl Et Me Cl Et Me Cl Et Me Cl Et Cl Cl Et Cl Cl Et ci ci Et Cl Cl Et Me Br Et Me Br Et Me Br Et Me Br Et Cl Br Et Cl Br Et Cl Br Et Cl Br Me Me H Me Me H Me Me H Me Me H Me Cl H Me Cl H Me Cl H Me Cl H Me Me Cl Me Me Cl Me Me CI Me Me Cl Me Cl Cl Me Cl Cl Me Cl Cl Me Cl Cl Me Me Br Me Me Br Me Me Br Me Me Br Me Cl Br Me Cl Br Me Cl Br Me Cl Br Table 20 R3 R4a R4b R5 R6 R3 R4a R4b R5 R6 R3 R4a R4b R5 R6 Me CH3 H CF3 Cl Me Cl H Cl Br Me Cl Br Cl Br Et CH3 H CF3 Cl Et Cl H Cl Br Et Cl Br Cl Br i-Pr CH3 H CF3 Cl i-Pr Cl H Cl Br i-Pr Cl Br Cl Br t-Bu CH3 H CF3 Cl t-Bu Cl H Cl Br t-Bu Cl Br Cl Br Me CH3 H CF3 Br Me CI H Br Cl Me Cl Br Br CI Et CH3 H CF3 Br Et Cl H Br Cl Et Cl Br Br Cl i-Pr CH3 H CF3 Br i-Pr CI H Br Cl i-Pr Cl Br Br Cl t-Bu CH3 H CF3 Br t-Bu Cl H Br Cl t-Bu Cl Br Br Cl Me CH3 H Cl Cl Me Cl H Br Br Me Cl Br Br Br Et CH3 H Cl Cl Et Cl H Br Br Et Cl Br Br Br i-Pr CH3 H Cl Cl i-Pr Cl H Br Br i-Pr Cl Br Br Br t-Bu CH3 H Cl Cl t-Bu Cl H Br Br t-Bu Cl Br Br Br Me CH3 H CI Br Me Cl H CF3 Cl Me Cl I CF3 Cl Et CH3 H Cl Br Et Cl H CF3 Cl Et Cl I CF3 Cl i-Pr CH3 H Cl Br i-Pr Cl H CF3 Cl i-Pr Cl I CF3 Cl t-Bu CH3 H Cl Br t-Bu Cl H CF3 Cl t-Bu Cl I CF3 Cl Me CH3 H Br Cl Me Cl H CF3 Br Me Cl I CF3 Br Et CH3 H Br Cl Et Cl H CF3 Br Et Cl I CF3 Br i-Pr CH3 H Br Cl i-Pr Cl H CF3 Br i-Pr Cl I CF3 Br t-Bu CH3 H Br Cl t-Bu Cl H CF3 Br t-Bu Cl I CF3 Br Me CH3 H Br Br Me Cl H Cl Cl Me Cl I Cl Cl Et CH3 H Br Br Et Cl H Cl Cl Et Cl I Cl Cl i-Pr CH3 H Br Br i-Pr Cl H Cl Cl i-Pr Cl I CI Cl t-Bu CH3 H Br Br i-Pr Cl H Cl Cl t-Bu Cl I Cl CI Me CH3 F CF3 Cl Me CH3 Cl CF3 Cl Me Cl I Cl Br Et CH3 F CF3 Cl Et CH3 Cl CF3 Cl Et Cl I Cl Br i-Pr CH3 F CF3 Cl i-Pr CH3 Cl CF3 Cl i-Pr Cl I Cl Br t-Bu CH3 F CF3 Cl t-Bu CH3 Cl CF3 Cl t-Bu Cl I Cl Br Me CH3 F CF3 Br Me CH3 Cl CF3 Br Me Cl I Br Cl R3 R4a R4b R5 R6 R3 R4a R4b R5 R6 R3 R4a R4b R5 R6 Et CH3 F CF3 Br Et CH3 Cl CF3 Br Et Cl I Br Cl i-Pr CH3 F CF3 Br i-Pr CH3 Cl CF3 Br i-Pr Cl I Br Cl t-Bu CH3 F CF3 Br t-Bu CH3 Cl CF3 Br t-Bu Cl I Br Cl Me CH3 F Cl Cl Me CH3 Cl Cl Cl Me Cl I Br Br Et CH3 F Cl Cl Et CH3 Cl Cl Cl Et Cl I Br Br i-Pr CH3 F Cl Cl i-Pr CH3 Cl Cl Cl i-Pr Cl I Br Br t-Bu CH3 F CI Cl t-Bu CH3 Cl Cl Cl t-Bu Cl I Br Br Me CH3 F Cl Br Me CH3 Cl Cl Br Me Cl CF3 CF3 Cl Et CH3 F CI Br Et CH3 Cl Cl Br Et Cl CF3 CF3 Cl i-Pr CH3 F Cl Br i-Pr CH3 Cl Cl Br i-Pr Cl CF3 CF3 Cl t-Bu CH3 F Cl Br t-Bu CH3 Cl Cl Br t-Bu Cl CF3 CF3 Cl Me CH3 F Br Cl Me CH3 Cl Br Cl Me Cl CF3 CF3 Br Et CH3 F Br CI Et CH3 Cl Br CI Et Cl CF3 CF3 Br i-Pr CH3 F Br Cl i-Pr CH3 Cl Br Cl i-Pr Cl CF3 CF3 Br t-Bu CH3 F Br Cl t-Bu CH3 Cl Br Cl t-Bu Cl CF3 CF3 Br Me CH3 F Br Br Me CH3 Cl Br Br Me Cl CF3 Cl Cl Et CH3 F Br Br Et CH3 Cl Br Br Et Cl CF3 Cl Cl i-Pr CH3 F Br Br i-Pr CH3 Cl Br Br i-Pr Cl CF3 Cl Cl t-Bu CH3 F Br Br t-Bu CH3 Cl Br Br T-Bu Cl CF3 Cl Cl Me CH3 Br CF3 Cl Me Cl F CF3 Cl Me Cl CF3 Cl Br Et CH3 Br CF3 Cl Et Cl F CF3 Cl Et Cl CF3 Cl Br i-Pr CH3 Br CF3 Cl i-Pr Cl F CF3 Cl i-Pr Cl CF3 Cl Br t-Bu CH3 Br CF3 Cl t-Bu Cl F CF3 Cl t-Bu Cl CF3 Cl Br Me CH3 Br CF3 Br Me Cl F CF3 Br Me Cl CF3 Br Cl Et CH3 Br CF3 Br Et Cl F CF3 Br Et Cl CF3 Br Cl i-Pr CH3 Br CF3 Br i-Pr Cl F CF3 Br i-Pr Cl CF3 Br Cl t-Bu CH3 Br CF3 Br t-Bu Cl F CF3 Br t-Bu Cl CF3 Br Cl Me CH3 Br Cl Cl Me Cl F Cl Cl Me Cl CF3 Br Br Et CH3 Br Cl Cl Et Cl F Cl Cl Et Cl CF3 Br Br i-Pr CH3 Br Cl Cl i-Pr Cl F Cl Cl i-Pr Cl CF3 Br Br t-Bu CH3 Br Cl Cl t-Bu Cl F Cl Cl t-Bu Cl CF3 Br Br Me CH3 Br Cl Br Me Cl F Cl Br n-Pr Cl Cl Cl Cl Et CH3 Br Cl Br Et Cl F Cl Br n-Bu Cl Cl Cl Cl i-Pr CH3 Br Cl Br i-Pr CI F Cl Br s-Bu Cl Cl Cl Cl t-Bu CH3 Br Cl Br t-Bu Cl F Cl Br i-Bu Cl Cl Cl Cl Me CH3 Br Br Cl Me Cl F Br Cl Me Br F CF3 Cl Et CH3 Br Br Cl Et Cl F Br Cl Et Br F CF3 Cl R3 R4a R4b R5 R6 R3 R4a R4b R5 R6 R3 R4a R4b R5 R6 i-Pr CH3 Br Br Cl i-Pr Cl F Br Cl i-Pr Br F CF3 Cl t-Bu CH3 Br Br Cl t-Bu Cl F Br Cl t-Bu Br F CF3 Cl Me CH3 Br Br Br Me Cl F Br Br Me Br F CF3 Br Et CH3 Br Br Br Et Cl F Br Br Et Br F CF3 Br i-Pr CH3 Br Br Br i-Pr Cl F Br Br i-Pr Br F CF3 Br t-Bu CH3 Br Br Br t-Bu Cl F Br Br t-Bu Br F CF3 Br Me CH3 I CF3 Cl Me Cl Cl CF3 Cl Me Br F Cl Ci Et CH3 I CF3 Cl Et Cl Cl CF3 Cl Et Br F Cl Cl i-Pr CH3 I CF3 Cl i-Pr Cl Cl CF3 Cl i-Pr Br F Cl Cl t-Bu CH3 I CF3 Cl t-Bu Cl Cl CF3 Cl t-Bu Br F Cl Cl Me CH3 I CF3 Br Me Cl Cl CF3 Br Me Br F Cl Br Et CH3 I CF3 Br Et Cl Cl CF3 Br Et Br F Cl Br i-Pr CH3 I CF3 Br i-Pr Cl Cl CF3 Br i-Pr Br F Cl Br t-Bu CH3 I CF3 Br t-Bu Cl Cl CF3 Br t-Bu Br F Cl Br Me CH3 I Cl Cl Me Cl Cl Cl Cl Me Br F Br Cl Et CH3 I Cl Cl Et Cl CI Cl Cl Et Br F Br Cl i-Pr CH3 I Cl Cl i-Pr Cl Cl Cl Cl i-Pr Br F Br CI t-Bu CH3 I Cl Cl t-Bu Cl Cl Cl Cl t-Bu Br F Br Cl Me CH3 I Cl Br Me Cl Cl Cl Br Me Br F Br Br Et CH3 I Cl Br Et Cl Cl Cl Br Et Br F Br Br i-Pr CH3 I Cl Br i-Pr Cl Cl Cl Br i-Pr Br F Br Br t-Bu CH3 I Cl Br t-Bu Cl Cl Cl Br t-Bu Br F Br Br Me CH3 I Br Cl Me Br CF3 CF3 Cl Me Br Cl CF3 Cl Et CH3 I Br Cl Et Br CF3 CF3 Cl Et Br Cl CF3 Cl i-Pr CH3 I Br Cl i-Pr Br CF3 CF3 Cl i-Pr Br Cl CF3 Cl t-Bu CH3 I Br Cl t-Bu Br CF3 CF3 Cl t-Bu Br Cl CF3 Cl Me CH3 I Br Br Me Br CF3 CF3 Br Me Br Cl CF3 Br Et CH3 I Br Br Et Br CF3 CF3 Br Et Br Cl CF3 Br i-Pr CH3 I Br Br i-Pr Br CF3 CF3 Br i-Pr Br Cl CF3 Br t-Bu CH3 I Br Br t-Bu Br CF3 CF3 Br t-Bu Br Cl CF3 Br Me CH3 CF3 CF3 Cl Me Br CF3 Cl Cl Me Br Cl Cl Cl Et CH3 CF3 CF3 Cl Et Br CF3 Cl Cl Et Br Cl Cl Cl i-Pr CH3 CF3 CF3 Cl i-Pr Br CF3 Cl Cl i-Pr Br Cl Cl Cl t-Bu CH3 CF3 CF3 Cl t-Bu Br CF3 Cl Cl t-Bu Br CI Cl Cl Me CH3 CF3 CF3 Br Me Br CF3 Cl Br Me Br Cl Cl Br Et CH3 CF3 CF3 Br Et Br CF3 Cl Br Et Br Cl Cl Br i-Pr CH3 CF3 CF3 Br i-Pr Br CF3 Cl Br i-Pr Br Cl Cl Br R3 R4a R4b R5 R6 R3 R4a R4b R5 R6 R3 R4a R4b R5 R6 t-Bu CH3 CF3 CF3 Br t-Bu Br CF3 Cl Br t-Bu Br Cl Cl Br Me CH3 CF3 Cl Cl Me Br CF3 Br Cl Me Br Cl Br Cl Et CH3 CF3 Cl Cl Et Br CF3 Br Cl Et Br CI Br Cl i-Pr CH3 CF3 Cl Cl i-Pr Br CF3 Br Cl i-Pr Br Cl Br Cl t-Bu CH3 CF3 Cl Cl t-Bu Br CF3 Br Cl t-Bu Br Cl Br Cl Me CH3 CF3 Cl Br Me Br CF3 Br Br Me Br Cl Br Br Et CH3 CF3 Cl Br Et Br CF3 Br Br Et Br Cl Br Br i-Pr CH3 CF3 Cl Br i-Pr Br CF3 Br Br i-Pr Br Cl Br Br t-Bu CH3 CF3 Cl Br t-Bu Br CF3 Br Br t-Bu Br Cl Br Br Me CH3 CF3 Br Cl Me Br I CF3 Cl Me Br Br CF3 Cl Et CH3 CF3 Br Cl Et Br I CF3 Cl Et Br Br CF3 Cl i-Pr CH3 CF3 Br Cl i-Pr Br I CF3 Cl i-Pr Br Br CF3 Cl t-Bu CH3 CF3 Br Cl t-Bu Br I CF3 Cl t-Bu Br Br CF3 Cl Me CH3 CF3 Br Br Me Br I CF3 Br Me Br Br CF3 Br Et CH3 CF3 Br Br Et Br I CF3 Br Et Br Br CF3 Br i-Pr CH3 CF3 Br Br i-Pr Br I CF3 Br i-Pr Br Br CF3 Br t-Bu CH3 CF3 Br Br t-Bu Br I CF3 Br t-Bu Br Br CF3 Br n-Pr CH3 Cl Cl Cl Me Br I Cl Cl Me Br Br Cl Cl n-Bu CH3 Cl Cl Cl Et Br I Cl Cl Et Br Br Cl Cl s-Bu CH3 Cl Cl Cl i-Pr Br I Cl Cl i-Pr Br Br Cl Cl i-Bu CH3 Cl Cl Cl t-Bu Br I Cl Cl t-Bu Br Br Cl CI Me Cl Cl Br Cl Me Br I Cl Br Me Br Br Cl Br Et Cl Cl Br Cl Et Br I Cl Br Et Br Br Cl Br i-Pr Cl Cl Br Cl i-Pr Br I Cl Br i-Pr Br Br Cl Br t-Bu Cl Cl Br Cl t-Bu Br I Cl Br t-Bu Br Br Cl Br Me Cl Cl Br Br Me Br I Br Cl Me Br Br Br Cl Et Cl Cl Br Br Et Br I Br CI Et Br Br Br Cl i-Pr Cl Cl Br Br i-Pr Br I Br Cl i-Pr Br Br Br Cl t-Bu Cl Cl Br Br t-Bu Br I Br Cl t-Bu Br Br Br Cl Me Cl Br CF3 Cl Me Br I Br Br Me Br Br Br Br Et Cl Br CF3 Cl Et Br I Br Br Et Br Br Br Br i-Pr Cl Br CF3 Cl i-Pr Br I Br Br i-Pr Br Br Br Br t-Bu Cl Br CF3 Cl t-Bu Br I Br Br t-Bu Br Br Br Br Me Cl Br CF3 Br Me Cl Br Cl Cl t-Bu Cl Br CF3 Br Et Cl Br CF3 Br Et Cl Br Cl Cl t-Bu Cl Br Cl Cl i-Pr Cl Br CF3 Br i-Pr Cl Br Cl Cl Table 21 R3 R4a R4b R5 R6 R3 R4a R4b R5 R6 R3 R4a R4b R5 R6 Me CH3 H CF3 Cl Me Ci F CF3 Cl Me Cl H Cl Br Et CH3 H CF3 Cl Et Cl F CF3 Cl Et Cl H Cl Br i-Pr CH3 H CF3 Cl i-Pr Cl F CF3 Cl i-Pr Cl H Cl Br t-Bu CH3 H CF3 Cl t-Bu Cl F CF3 Cl t-Bu Cl H Cl Br Me CH3 H CF3 Br Me Cl F CF3 Br Me Cl H Br Cl Et CH3 H CF3 Br Et Cl F CF3 Br Et Cl H Br Cl i-Pr CH3 H CF3 Br i-Pr Cl F CF3 Br i-Pr Cl H Br Cl t-Bu CH3 H CF3 Br t-Bu Cl F CF3 Br t-Bu Cl H Br Cl Me CH3 H Cl Cl Me Cl F Cl Cl Me Cl H Br Br Et CH3 H Cl Cl Et Cl F Cl Cl Et Cl H Br Br i-Pr CH3 H Cl Cl i-Pr Cl F Cl Cl i-Pr Cl H Br Br t-Bu CH3 H Cl Cl t-Bu Cl F Cl Cl t-Bu Cl H Br Br Me CH3 H Cl Br Me Cl F Cl Br Me Cl H CF3 Cl Et CH3 H Cl Br Et Cl F Cl Br Et Cl H CF3 Cl i-Pr CH3 H Cl Br i-Pr Cl F Cl Br i-Pr Cl H CF3 Cl t-Bu CH3 H Cl Br t-Bu Cl F Cl Br t-Bu Cl H CF3 Cl Me CH3 H Br Cl Me Cl F Br Cl Me Cl H CF3 Br Et CH3 H Br Cl Et Cl F Br CI Et CI H CF3 Br i-Pr CH3 H Br Cl i-Pr Cl F Br Cl i-Pr Cl H CF3 Br t-Bu CH3 H Br Cl t-Bu Cl F Br Cl t-Bu Cl H CF3 Br Me CH3 H Br Br Me Cl F Br Br Me Cl H Cl Cl Et CH3 H Br Br Et Cl F Br Br Et Cl H Cl Cl i-Pr CH3 H Br Br i-Pr Cl F Br Br i-Pr Cl H Cl Cl t-Bu CH3 H Br Br t-Bu Cl F Br Br i-Pr Cl H Cl Cl Me CH3 F CF3 Cl Me Cl Cl CF3 Cl Me Cl Br Cl Br Et CH3 F CF3 Cl Et Cl Cl CF3 Cl Et Cl Br Cl Br i-Pr CH3 F CF3 Cl i-Pr Cl Cl CF3 Cl i-Pr Cl Br Cl Br t-Bu CH3 F CF3 Cl t-Bu Cl Cl CF3 Cl t-Bu Cl Br Cl Br Me CH3 F CF3 Br Me Cl Cl CF3 Br Me CI Br Br Cl R3 R4a R4b R5 R6 R3 R4a R4b R5 R6 R3 R4a R4b R5 R6 Et CH3 F CF3 Br Et Cl Cl CF3 Br Et Cl Br Br ci i-Pr CH3 F CF3 Br i-Pr Cl Cl CF3 Br i-Pr Cl Br Br Cl t-Bu CH3 F CF3 Br t-Bu Cl Cl CF3 Br t-Bu Cl Br Br Cl Me CH3 F Cl Cl Me Cl Cl Cl Cl Me Cl Br Br Br Et CH3 F Cl Cl Et Cl Cl Cl Cl Et Cl Br Br Br i-Pr CH3 F Cl Cl i-Pr Cl Cl Cl Cl i-Pr Cl Br Br Br t-Bu CH3 F Cl Cl t-Bu Cl Cl Cl Cl t-Bu Cl Br Br Br Me CH3 F Cl Br Me Cl Cl Cl Br Me Cl I CF3 Cl Et CH3 F CI Br Et Cl Cl Cl Br Et Cl I CF3 Cl i-Pr CH3 F Cl Br i-Pr Cl Cl Cl Br i-Pr Cl I CF3 Cl t-Bu CH3 F Cl Br t-Bu Cl Cl Cl Br t-Bu Cl I CF3 Cl Me CH3 F Br Cl Me Cl Cl Br Cl Me Cl I CF3 Br Et CH3 F Br Cl Et Cl Cl Br CI Et Cl I CF3 Br i-Pr CH3 F Br Cl i-Pr Cl Cl Br Cl i-Pr Cl I CF3 Br t-Bu, CH3 F Br Cl t-Bu Cl Cl Br Cl t-Bu Cl I CF3 Br Me CH3 F Br Br Me Cl Cl Br Br Me Cl I Cl Cl Et CH3 F Br Br Et Cl Cl Br Br Et Cl I Cl Cl i-Pr CH3 F Br Br i-Pr Cl Cl Br Br i-Pr Cl I Cl Cl t-Bu CH3 F Br Br t-Bu Cl Cl Br Br t-Bu Cl I Cl Cl Me CH3 Cl CF3 Cl Me Cl Br CF3 Cl Me Cl I Cl Br Et CH3 Cl CF3 Cl Et Cl Br CF3 Cl Et Cl I Cl Br i-Pr CH3 Cl CF3 Cl i-Pr Cl Br CF3 Cl i-Pr Cl I Cl Br t-Bu CH3 Cl CF3 Cl t-Bu Cl Br CF3 Cl t-Bu Cl I Cl Br Me CH3 Cl CF3 Br Me Cl Br CF3 Br Me Cl I Br Cl Et CH3 Cl CF3 Br Et Cl Br CF3 Br Et Cl I Br Cl i-Pr CH3 Cl CF3 Br i-Pr Cl Br CF3 Br i-Pr Cl I Br CI t-Bu CH3 Cl CF3 Br t-Bu Cl Br CF3 Br t-Bu Cl I Br Cl Me CH3 Cl Cl Cl Me Cl Br Cl Cl Me Cl I Br Br Et CH3 Cl Cl Cl Et Cl Br Cl CI Et Cl I Br Br i-Pr CH3 Cl Cl Cl i-Pr Cl Br Cl Cl i-Pr Cl I Br Br t-Bu CH3 Cl Cl Cl t-Bu Cl Br Cl Cl t-Bu Cl I Br Br Me CH3 Cl Cl Br Me Br Br Br Cl Me Cl CF3 CF3 Cl Et CH3 Cl Cl Br Et Br Br Br Cl Et Cl CF3 CF3 Cl i-Pr CH3 Cl Cl Br i-Pr Br Br Br Cl i-Pr Cl CF3 CF3 Cl t-Bu CH3 Cl Cl Br t-Bu Br Br Br Cl t-Bu Cl CF3 CF3 Cl Me CH3 Cl Br Cl Me Br Br Br Br Me Cl CF3 CF3 Br Et CH3 Cl Br Cl Et Br Br Br Br Et Cl CF3 CF3 Br R3 R4a R4b R5 R6 R3 R4a R4b R5 R6 R3 R4a R4b R5 R6 i-Pr CH3 Cl Br Cl i-Pr Br Br Br Br i-Pr Cl CF3 CF3 Br t-Bu CH3 Cl Br Cl t-Bu Br Br Br Br t-Bu Cl CF3 CF3 Br Me CH3 Cl Br Br Me Br I CF3 Cl Me Cl CF3 Cl Cl Et CH3 Cl Br Br Et Br I CF3 Cl Et Cl CF3 Cl Cl i-Pr CH3 Cl Br Br i-Pr Br I CF3 Cl i-Pr Cl CF3 Cl Cl t-Bu CH3 Cl Br Br t-Bu Br I CF3 Cl t-Bu Cl CF3 Cl Cl Me CH3 Br CF3 Cl Me Br I CF3 Br Me Cl CF3 Cl Br Et CH3 Br CF3 Cl Et Br I CF3 Br Et Cl CF3 Cl Br i-Pr CH3 Br CF3 Cl i-Pr Br I CF3 Br i-Pr Cl CF3 Cl Br t-Bu CH3 Br CF3 Cl t-Bu Br I CF3 Br t-Bu Cl CF3 Cl Br Me CH3 Br CF3 Br Me Br I Cl Cl Me Cl CF3 Br Cl Et CH3 Br CF3 Br Et Br I Cl Cl Et Cl CF3 Br Cl i-Pr CH3 Br CF3 Br i-Pr Br I Cl Cl i-Pr Cl CF3 Br Cl t-Bu CH3 Br CF3 Br t-Bu Br I Cl Cl t-Bu Cl CF3 Br Cl Me CH3 Br Cl Cl Me Br I Cl Br Me Cl CF3 Br Br Et CH3 Br Cl Cl Et Br I Cl Br Et Cl CF3 Br Br i-Pr CH3 Br Cl Cl i-Pr Br I Cl Br i-Pr Cl CF3 Br Br t-Bu CH3 Br Cl Cl t-Bu Br I Cl Br t-Bu Cl CF3 Br Br Me CH3 Br Cl Br Me Br I Br Cl n-pur Cl Cl Cl Cl Et CH3 Br Cl Br Et Br I Br Cl rr-Bu Cl Cl Cl Cl i-Pr CH3 Br Cl Br i-Pr Br I Br Cl s-Bu Cl Cl Cl Cl t-Bu CH3 Br Cl Br t-Bu Br I Br Cl t-Bu Cl Cl Cl Cl Me CH3 Br Br Cl Me Br I Br Br Me Br F CF3 Cl Et CH3 Br Br Cl Et Br I Br Br Et Br F CF3 Cl i-Pr CH3 Br Br Cl i-Pr Br I Br Br i-Pr Br F CF3 Cl t-Bu CH3 Br Br Cl t-Bu Br I Br Br t-Bu Br F CF3 Cl Me CH3 Br Br Br Me Br CF3 CF3 Cl Me Br F CF3 Br Et CH3 Br Br Br Et Br CF3 CF3 Cl Et Br F CF3 Br i-Pr CH3 Br Br Br i-Pr Br CF3 CF3 Cl i-Pr Br F CF3 Br t-Bu CH3 Br Br Br t-Bu Br CF3 CF3 Cl t-Bu Br F CF3 Br Me CH3 I CF3 Cl Me Br CF3 CF3 Br Me Br F Cl Cl Et CH3 I CF3 Cl Et Br CF3 CF3 Br Et Br F CI Cl i-Pr CH3 I CF3 Cl i-Pr Br CF3 CF3 Br i-Pr Br F Cl Cl t-Bu CH3 I CF3 Cl t-Bu Br CF3 CF3 Br t-Bu Br F Cl CI Me CH3 I CF3 Br Me Br CF3 Cl Cl Me Br F Cl Br Et CH3 I CF3 Br Et Br CF3 Cl Cl Et Br F Cl Br i-Pr CH3 I CF3 Br i-Pr Br CF3 Cl Cl i-Pr Br F Cl Br R3 R4a R4b R5 R6 R3 R4a R4b R5 R6 R3 R4a R4b R5 R6 t-Bu CH3 I CF3 Br t-Bu Br CF3 Cl Cl t-Bu Br F Cl Br Me CH3 I Cl Cl Me Br CF3 Cl Br Me Br F Br Cl Et CH3 I Cl Cl Et Br CF3 Cl Br Et Br F Br Cl i-Pr CH3 I Cl Cl i-Pr Br CF3 Cl Br i-Pr Br F Br Cl t-Bu CH3 I Cl Cl t-Bu Br CF3 Cl Br t-Bu Br F Br Cl Me CH3 I Cl Br Me Br CF3 Br Cl Me Br F Br Br Et CH3 I Cl Br Et Br CF3 Br Cl Et Br F Br Br i-Pr CH3 I Cl Br i-Pr Br CF3 Br Cl i-Pr Br F Br Br t-Bu CH3 I Cl Br t-Bu Br CF3 Br Cl t-Bu Br F Br Br Me CH3 I Br Cl Me Br CF3 Br Br Me Br Cl CF3 Cl Et CH3 I Br Cl Et Br CF3 Br Br Et Br Cl CF3 CI i-Pr CH3 I Br Cl i-Pr Br CF3 Br Br i-Pr Br Cl CF3 Cl t-Bu CH3 I Br Cl t-Bu Br CF3 Br Br t-Bu Br Cl CF3 Cl Me CH3 I Br Br Me Br Br CF3 Cl Me Br Cl CF3 Br Et CH3 I Br Br Et Br Br CF3 Cl Et Br Cl CF3 Br i-Pr CH3 I Br Br i-Pr Br Br CF3 Cl i-Pr Br Cl CF3 Br t-Bu CH3 I Br Br t-Bu Br Br CF3 Cl t-Bu Br Cl CF3 Br Me CH3 CF3 CF3 Cl Me Br Br CF3 Br Me Br Cl CI Cl Et CH3 CF3 CF3 Cl Et Br Br CF3 Br Et Br Cl Cl CI i-Pr CH3 CF3 CF3 Cl i-Pr Br Br CF3 Br i-Pr Br Cl Cl Cl t-Bu CH3 CF3 CF3 Cl t-Bu Br Br CF3 Br t-Bu Br Cl Cl Cl Me CH3 CF3 CF3 Br Me Br Br Cl Cl Me Br Cl Cl Br Et CH3 CF3 CF3 Br Et Br Br Cl Cl Et Br Cl Cl Br i-Pr CH3 CF3 CF3 Br i-Pr Br Br Cl Cl i-Pr Br Cl Cl Br t-Bu CH3 CF3 CF3 Br t-Bu Br Br Cl Cl t-Bu Br Cl Cl Br Me CH3 CF3 Cl Cl Me Br Br Cl Br Me Br Cl Br Cl Et CH3 CF3 Cl Cl Et Br Br Cl Br Et Br Cl Br Cl i-Pr CH3 CF3 Cl Cl i-Pr Br Br Cl Br i-Pr Br Cl Br Cl t-Bu CH3 CF3 Cl Cl t-Bu Br Br Cl Br t-Bu Br Cl Br CI Me CH3 CF3 Cl Br Me CH3 CF3 Br Cl Me Br Cl Br Br Et CH3 CF3 Cl Br Et CH3 CF3 Br Cl Et Br Cl Br Br i-Pr CH3 CF3 Cl Br i-Pr CH3 CF3 Br Cl i-Pr Br Cl Br Br t-Bu CH3 CF3 Cl Br t-Bu CH3 CF3 Br Cl t-Bu Br Cl Br Br Me CH3 CF3 Br Br n-Pr CH3 Cl Cl Cl t-Bu CH3 CF3 Br Br Et CH3 CF3 Br Br n-Bu CH3 Cl Cl Cl i-Bu CH3 Cl Cl Cl i-Pr CH3 CF3 Br Br s-Bu CH3 Cl Cl Cl Table 22 R5b is CHF2 R5b is CF3 R5b is CH2CF3 R5b is CF2CHF2 R3 R4a R4b R3 R4a R4b R3 R4a R4b R3 R4a R4b i-Pr Me H i-Pr Me H i-Pr Me H i-Pr Me H i-Pr Cl H i-Pr Cl H i-Pr Cl H i-Pr Cl H i-Pr Me Cl i-Pr Me Cl i-Pr Me Cl i-Pr Me Cl i-Pr Cl Cl i-Pr Cl Cl i-Pr Cl Cl i-Pr Cl Cl i-Pr Me Br i-Pr Me Br i-Pr Me Br i-Pr Me Br i-Pr Cl Br i-Pr Cl Br i-Pr Cl Br i-Pr Cl Br t-Bu Me H t-Bu Me H t-Bu Me H t-Bu Me H t-Bu Cl H t-Bu Cl H t-Bu Cl H t-Bu Cl H t-Bu Me Cl t-Bu Me Cl t-Bu Me Cl t-Bu Me Cl t-Bu Cl Cl t-Bu Cl Cl t-Bu Cl Cl t-Bu Cl Cl t-Bu Me Br t-Bu Me Br t-Bu Me Br t-Bu Me Br t-Bu Cl Br t-Bu Cl Br t-Bu Cl Br t-Bu Cl Br Et Me H Et Me H Et Me H Et Me H Et Cl H Et Cl H Et Cl H Et Cl H Et Me Ci Et Me Cl Et Me Cl Et Me Cl Et CI Cl Et Cl Cl Et Cl Cl Et Cl Cl Et Me Br Et Me Br Et Me Br Et Me Br Et Cl Br Et Cl Br Et Cl Br Et Cl Br Me Me H Me Me H Me Me H Me Me H Me Cl H Me Cl H Me Cl H Me Cl H Me Me Cl Me Me Cl Me Me Cl Me Me Cl Me Cl Cl Me Cl Cl Me Cl Cl Me Cl Cl Me Me Br Me Me Br Me Me Br Me Me Br Me Cl Br Me Cl Br Me Cl Br Me Cl Br Table 23 R5b is CHF2 R5b is CF3 R5b is CH2CVF3 R5b is CF2CHF2 R3 R4a R4b R3 R4a R4b R3 R4a R4b R3 R4a R4b i-Pr Me H i-Pr Me H i-Pr Me H i-Pr Me H i-Pr Cl H i-Pr Cl H i-Pr Cl H i-Pr Cl H i-Pr Me Cl i-Pr Me Cl i-Pr Me Cl i-Pr Me Cl i-Pr Cl Cl i-Pr CI Cl i-Pr Cl Cl i-Pr Cl Cl i-Pr Me Br i-Pr Me Br i-Pr Me Br i-Pr Me Br i-Pr Cl Br i-Pr Cl Br i-Pr Cl Br i-Pr Cl Br t-Bu Me H t-Bu Me H t-Bu Me H t-Bu Me H t-Bu Cl H t-Bu Cl H t-Bu Cl H t-Bu Cl H t-Bu Me Cl t-Bu Me Cl t-Bu Me Cl t-Bu Me Cl t-Bu Cl Cl t-Bu Cl Cl t-Bu Cl Cl t-Bu Cl Cl t-Bu Me Br t-Bu Me, Br t-Bu Me Br t-Bu Me Br t-Bu Cl Br t-Bu Cl Br t-Bu CI Br t-Bu CI Br Et Me H Et Me H Et Me H Et Me H Et Cl H Et Cl H Et CI H Et cl H Et Me Cl Et Me Cl Et Me Cl Et Me Cl Et CI Cl Et CI CI Et Cl ci Et Cl Cl Et Me Br Et Me Br Et Me Br Et Me Br Et Cl Br Et Cl Br Et Cl Br Et Cl Br Me Me H Me Me H Me Me H Me Me H Me CI H Me Cl H Me Cl H Me CI H Me Me Cl Me Me Cl Me Me Cl Me Me Cl Me Cl Cl Me Cl Cl Me Cl Cl Me Cl CI Me Me Br Me Me Br Me Me Br Me Me Br Me CI Br Me Cl Br Me Cl Br Me Cl Br Table 24 R5 is CHF2 R5 is CH2CF3 R5 is CH2CHF2 R3 R4a R4b R6 R3 R4a R4b R6 R3 R4a R4b R6 Me CH3 H Cl Me CH3 H Cl Me CH3 H Cl Et CH3 H Cl Et CH3 H Cl Et CH3 H Cl i-Pr CH3 H Cl i-Pr CH3 H Cl i-Pr CH3 H Cl t-Bu CH3 H CI t-Bu CH3 H Cl t-Bu CH3 H Cl Me CH3 H Br Me CH3 H Br Me CH3 H Br Et CH3 H Br Et CH3 H Br Et CH3 H Br i-Pr CH3 H Br i-Pr CH3 H Br i-Pr CH3 H Br t-Bu CH3 H Br t-Bu CH3 H Br t-Bu CH3 H Br Me CH3 F Cl Me CH3 F Cl Me CH3 F Cl Et CH3 F Cl Et CH3 F ci Et CH3 F Cl i-Pr CH3 F Cl i-Pr CH3 F Cl i-Pr CH3 F Cl t-Bu CH3 F Cl t-Bu CH3 F Cl t-Bu CH3 F Cl Me CH3 F Br Me CH3 F Br Me CH3 F Br Et CH3 F Br Et CH3 F Br Et CH3 F Br i-Pr CH3 F Br i-Pr CH3 F Br i-Pr CH3 F Br t-Bu CH3 F Br t-Bu CH3 F Br t-Bu CH3 F Br Me CH3 Cl Cl Me CH3 Cl Cl Me CH3 Cl CI Et CH3 Cl Cl Et CH3 Cl Cl Et CH3 Cl Cl i-Pr CH3 Cl Cl i-Pr CH3 Cl Cl i-Pr CH3 Cl Cl t-Bu CH3 Cl Cl t-Bu CH3 Cl Cl t-Bu CH3 Cl Cl Me CH3 Cl Br Me CH3 CI Br Me CH3 Cl Br Et CH3 Cl Br Et CH3 Cl Br Et CH3 Cl Br i-Pr CH3 CI Br i-Pr CH3 Cl Br i-Pr CH3 Cl Br t-Bu CH3 Cl Br t-Bu CH3 Cl Br t-Bu CH3 Cl Br Me CH3 Br Cl Me CH3 Br Cl Me CH3 Br Cl Et CH3 Br Cl Et CH3 Br Cl Et CH3 Br Cl i-Pr CH3 Br Cl i-Pr CH3 Br Cl i-Pr CH3 Br Cl t-Bu CH3 Br Cl t-Bu CH3 Br CI t-Bu CH3 Br Cl R5 is CHF2 R5 is CH2CF3 R5 is CF2CHF2 R3 R4a R4b R6 R3 R4a R4b R6 R3 R4a R4b R6 Me CH3 Br Br Me CH3 Br Br Me CH3 Br Br Et CH3 Br Br Et CH3 Br Br Et CH3 Br Br i-Pr CH3 Br Br i-Pr CH3 Br Br i-Pr CH3 Br Br t-Bu CH3 Br Br t-Bu CH3 Br Br t-Bu CH3 Br Br Me CH3 I Cl Me CH3 I Cl Me CH3 I Cl Et CH3 I Ci Et CH3 I Cl Et CH3 I Cl i-Pr CH3 I Cl i-Pr CH3 I Cl i-Pr CH3 I Cl t-Bu CH3 I Cl t-Bu CH3 I Cl t-Bu CH3 I Cl Me CH3 I Br Me CH3 I Br Me CH3 I Br Et CH3 I Br Et CH3 I Br Et CH3 I Br i-Pr CH3 I Br i-Pr CH3 I Br i-Pr CH3 I Br t-Bu CH3 I Br t-Bu CH3 I Br t-Bu CH3 I Br Me CH3 CF3 Cl Me CH3 CF3 Cl Me CH3 CF3 Cl Et CH3 CF3 Cl Et CH3 CF3 Cl Et CH3 CF3 Cl i-Pr CH3 CF3 Cl i-Pr CH3 CF3 Cl i-Pr CH3 CF3 Cl t-Bu CH3 CF3 Cl t-Bu CH3 CF3 Cl t-Bu CH3 CF3 Cl Me CH3 CF3 Br Me CH3 CF3 Br Me CH3 CF3 Br Et CH3 CF3 Br Et CH3 CF3 Br Et CH3 CF3 Br i-Pr CH3 CF3 Br i-Pr CH3 CF3 Br i-Pr CH3 CF3 Br t-Bu CH3 CF3 Br t-Bu CH3 CF3 Br t-Bu CH3 CF3 Br n-Pr CH3 Cl Cl Me Cl F Br Me Cl H Br n-Bu CH3 Cl Cl Et Cl F Br Et Cl H Br s-Bu CH3 Cl Cl i-Pr Cl F Br i-Pr Cl H Br i-Bu CH3 Cl Cl t-Bu Cl F Br t-Bu Cl H Br Me Cl F Cl Me Cl F Cl Me Cl H Cl Et ci F Cl Et Cl F Cl Et Cl H Cl i-Pr Cl F Cl i-Pr Cl F CI i-Pr Cl H Cl t-Bu Cl F Cl t-Bu Cl F Cl i-Pr Cl H Cl Me Cl F Br Me Cl Cl Br Me Cl I Br Et Cl F Br Et CI Cl Br Et Cl I Br i-Pr Cl F Br i-Pr Cl Cl Br i-Pr Cl I Br t-Bu Cl F Br t-Bu Cl Cl Br t-Bu Cl I Br Me Cl Cl Cl Me Cl Cl Cl Me Cl I Cl Et Cl Cl Cl Et Cl Cl Cl Et Cl I Cl i-Pr Cl Cl Cl i-Pr Cl Cl Cl i-Pr Cl I Cl t-Bu Cl Cl Cl t-Bu Cl Cl Cl t-Bu Cl I Cl R5 is CHF2 R5 is CH2CF3 R5 is CF2CHF2 R3 R4a R4b R6 R3 R4a R4b R6 R3 R4a R4b R6 Me Cl H Br Me Cl H Br Me Cl F Br Et CI H Br Et Cl H Br Et Cl F Br i-Pr Cl H Br i-Pr Cl H Br i-Pr Cl F Br t-Bu CI H Br t-Bu Cl H Br t-Bu Cl F Br Me Cl H Cl Me Cl H Cl Me Cl F Cl Et Cl H Cl Et Cl H Cl Et Cl F Cl i-Pr Cl H Cl i-Pr Cl H Cl i-Pr Cl F Cl t-Bu Cl H Cl t-Bu Cl H Cl t-Bu Cl F CI Me Cl Br Br Me Cl Br Br Me Cl CF3 Br Et CI Br Br Et Cl Br Br Et Cl CF3 Br i-Pr Cl Br Br i-Pr Cl Br Br i-Pr Cl CF3 Br t-Bu Cl Br Br t-Bu Cl Br Br t-Bu Cl CF3 Br Me Cl Br Cl Me Cl I Cl Me Cl CF3 Cl Et CI Br Cl Et Cl I Cl Et Cl CF3 Cl i-Pr Cl Br Cl i-Pr Cl I Cl i-Pr Cl CF3 Cl t-Bu Cl Br Cl t-Bu Cl I Cl t-Bu Cl CF3 Cl Me Cl I Br Me Cl I Br Me Br F Cl Et Cl I Br Et Cl I Br Et Br F Cl i-Pr Cl I Br i-Pr Cl I Br i-Pr Br F Cl t-Bu Cl I Br t-Bu Cl I Br t-Bu Br F Cl Me Cl I Cl Me Cl CF3 Cl Me Br F Br Et Cl I Cl Et Cl CF3 Cl Et Br F Br i-Pr Cl I Cl i-Pr Cl CF3 Cl i-Pr Br F Br t-Bu Cl I Cl t-Bu Cl CF3 Cl t-Bu Br F Br Me Cl CF3 Br Me Cl CF3 Br Me Br Cl Cl Et Cl CF3 Br Et Cl CF3 Br Et Br Cl Cl i-Pr Cl CF3 Br i-Pr Cl CF3 Br i-Pr Br Cl Cl t-Bu Cl CF3 Br t-Bu Cl CF3 Br t-Bu Br Cl Cl Me CI CF3 CI n-Pr Cl Cl Cl Me Br Cl Br Et Cl CF3 Cl n-Bu CI Cl Cl Et Br Cl Br i-Pr Cl CF3 Cl s-Bu Cl Cl Cl i-Pr Br Cl Br t-Bu Cl CF3 Cl i-Bu CI Cl Cl t-Bu Br Cl Br Me Br F Cl Me Br F Cl Me Br Br Cl Et Br F Cl Et Br F Cl Et Br Br Cl i-Pr Br F Cl i-Pr Br F Cl i-Pr Br Br Cl t-Bu Br F Cl t-Bu Br F Cl t-Bu Br Br Cl R5 is CHF2 R5 is CH2CF3 R5 is CF2CHF2 R3 R4a R4b R6 R3 R4a R4b R6 R3 R4a R4b R6 Me Br F Br Me Br F Br Me Br Br Br Et Br F Br Et Br F Br Et Br Br Br i-Pr Br F Br i-Pr Br F Br i-Pr Br Br Br t-Bu Br F Br t-Bu Br F Br t-Bu Br Br Br Me Br Cl CI Me Br Cl CI Me Br I Cl Et Br Cl Cl Et Br Cl Cl Et Br I Cl i-Pr Br Cl Cl i-Pr Br Cl Cl i-Pr Br I CI t-Bu Br Cl Cl t-Bu Br Cl Cl t-Bu Br I Cl Me Br Cl Br Me Br Cl Br Me Br I Br Et Br Cl Br Et Br Cl Br Et Br I Br i-Pr Br Cl Br i-Pr Br CI Br i-Pr Br I Br t-Bu Br Cl Br t-Bu Br Cl Br t-Bu Br I Br Me Br Br Cl Me Br Br Cl Me Br CF3 Cl Et Br Br Cl Et Br Br Cl Et Br CF3 Cl i-Pr Br Br Cl i-Pr Br Br Cl i-Pr Br CF3 Cl t-Bu Br Br Cl t-Bu Br Br Cl t-Bu Br CF3 Cl Me Br Br Br Me Br Br Br Me Br CF3 Br Et Br Br Br Et Br Br Br Et Br CF3 Br i-Pr Br Br Br i-Pr Br Br Br i-Pr Br CF3 Br t-Bu Br Br Br t-Bu Br Br Br t-Bu Br CF3 Br Me Br I Cl Me Br I Cl Me Cl Cl Br Et Br I ci Et Br I Cl Et Cl Cl Br i-Pr Br I Cl i-Pr Br I Cl i-Pr Cl Cl Br t-Bu Br I Cl t-Bu Br I Cl t-Bu Cl Cl Br Me Br I Br Me Br I Br Me Cl Cl Cl Et Br I Br Et Br I Br Et Cl Cl Cl i-Pr Br I Br i-Pr Br I Br i-Pr Cl Cl Cl t-Bu Br I Br t-Bu Br I Br t-Bu Cl Cl Cl Table 25 R5 is CHF2 R5 is CH2CF3 R5 is CF2CHF2 R3 R4a R4b R6 R3 R4a R4b R6 R3 R4a R4b R6 Me CH3 H Cl Me CH3 H Cl Me CH3 H Cl Et CH3 H Cl Et CH3 H Cl Et CH3 H Cl i-Pr CH3 H Cl i-Pr CH3 H Cl i-Pr CH3 H Cl t-Bu CH3 H Cl t-Bu CH3 H Cl t-Bu CH3 H Cl Me CH3 H Br Me CH3 H Br Me CH3 H Br Et CH3 H Br Et CH3 H Br Et CH3 H Br i-Pr CH3 H Br i-Pr CH3 H Br i-Pr CH3 H Br t-Bu CH3 H Br t-Bu CH3 H Br t-Bu CH3 H Br Me CH3 F Cl Me CH3 F Cl Me CH3 F Cl Et CH3 F Cl Et CH3 F Cl Et CH3 F Cl i-Pr CH3 F Cl i-Pr CH3 F Cl i-Pr CH3 F Cl t-Bu CH3 F Cl t-Bu CH3 F Cl t-Bu CH3 F Cl Me CH3 F Br Me CH3 F Br Me CH3 F Br Et CH3 F Br Et CH3 F Br Et CH3 F Br i-Pr CH3 F Br i-Pr CH3 F Br i-Pr CH3 F Br t-Bu CH3 F Br t-Bu CH3 F Br t-Bu CH3 F Br Me CH3 Cl Cl Me CH3 Cl Cl Me CH3 Cl Cl Et CH3 Cl Cl Et CH3 Cl Cl Et CH3 Cl Cl i-Pr CH3 Cl Cl i-Pr CH3 Cl Cl i-Pr CH3 Cl Cl t-Bu CH3 Cl Cl t-Bu CH3 Cl Cl t-Bu CH3 Cl Cl Me CH3 Cl Br Me CH3 Cl Br Me CH3 Cl Br Et CH3 Ci Br Et CH3 Cl Br Et CH3 Cl Br i-Pr CH3 Cl Br i-Pr CH3 Cl Br i-Pr CH3 Cl Br t-Bu CH3 Cl Br t-Bu CH3 Cl Br t-Bu CH3 Cl Br Me CH3 Br Cl Me CH3 Br Cl Me CH3 Br Cl Et CH3 Br Cl Et CH3 Br Cl Et CH3 Br Cl i-Pr CH3 Br Cl i-Pr CH3 Br Cl i-Pr CH3 Br Cl t-Bu CH3 Br Cl t-Bu CH3 Br Cl t-Bu CH3 Br Cl Me CH3 Br Br Me CH3 Br Br Me CH3 Br Br R5 is CHF2 R5 is CH2CF3 E5 is CF2CHF2 R3 R4a R4b R6 R3 R4a R4b R6 R3 R4a R4b R6 Et CH3 Br Br Et CH3 Br Br Et CH3 Br Br i-Pr CH3 Br Br i-Pr CH3 Br Br i-Pr CH3 Br Br t-Bu CH3 Br Br t-Bu CH3 Br Br t-Bu CH3 Br Br Me CH3 I Cl Me CH3 I Cl Me CH3 I Cl Et CH3 I Cl Et CH3 I Cl Et CH3 I Ci i-Pr CH3 I Cl i-Pr CH3 I Cl i-Pr CH3 I Cl t-Bu CH3 I Cl t-Bu CH3 I Cl t-Bu CH3 I Cl Me CH3 I Br Me CH3 I Br Me CH3 I Br Et CH3 I Br Et CH3 I Br Et CH3 I Br i-Pr CH3 I Br i-Pr CH3 I Br i-Pr CH3 I Br t-Bu CH3 I Br t-Bu CH3 I Br t-Bu CH3 I Br Me CH3 CF3 Cl Me CH3 CF3 Cl Me CH3 CF3 Cl Et CH3 CF3 Cl Et CH3 CF3 Cl Et CH3 CF3 Cl i-Pr CH3 CF3 Cl i-Pr CH3 CF3 Cl i-Pr CH3 CF3 Cl t-Bu CH3 CF3 Cl t-Bu CH3 CF3 Cl t-Bu CH3 CF3 Cl Me CH3 CF3 Br Me CH3 CF3 Br Me CH3 CF3 Br Et CH3 CF3 Br Et CH3 CF3 Br Et CH3 CF3 Br i-Pr CH3 CF3 Br i-Pr CH3 CF3 Br i-Pr CH3 CF3 Br t-Bu CH3 CF3 Br t-Bu CH3 CF3 Br t-Bu CH3 CF3 Br n-Pr CH3 Cl Cl Me Cl F Br Me Cl H Br n-Bu CH3 Cl Cl Et Cl F Br Et Cl H Br s-Bu CH3 CI Cl i-Pr Cl F Br i-Pr Cl H Br i-Bu CH3 Cl Cl t-Bu Cl F Br t-Bu Cl H Br Me Cl F Cl Me CI F Cl Me Cl H Cl Et Cl F Cl Et Cl F Cl Et Cl H Cl i-Pr Cl F Cl i-Pr Cl F Cl i-Pr Cl H Cl t-Bu Cl F Cl t-Bu Cl F Cl i-Pr Cl H Cl Me Cl F Br Me CI Cl Br Me Cl I Br Et Cl F Br Et Cl Cl Br Et Cl I Br i-Pr Cl F Br i-Pr Cl Cl Br i-Pr Cl I Br t-Bu Cl F Br t-Bu Cl Cl Br t-Bu Cl I Br Me Cl Cl Cl Me Cl Cl Cl Me Cl I Cl Et CI Cl Cl Et Cl Cl Cl Et Cl I Cl i-Pr Cl Cl Cl i-Pr Cl Cl Cl i-Pr Cl I CI t-Bu Cl Cl Cl t-Bu CI Cl Cl t-Bu Cl I Cl Me Cl H Br Me Cl H Br Me Cl F Br R5 is CHF2 R5 is CH2CF3 R5 is CF2CHF2 R3 R4a R4b R6 R3 R4a R4b R6 R3 R4a R4b R6 Et Cl H Br Et Cl H Br Et Cl F Br i-Pr Cl H Br i-Pr Cl H Br i-Pr Cl F Br t-Bu Cl H Br t-Bu Cl H Br t-Bu Cl F Br Me Cl H Cl Me ci H Cl Me Cl F Cl Et Cl H Cl Et Cl H Cl Et Cl F Cl i-Pr Cl H Cl i-Pr Cl H Cl i-Pr Cl F Cl t-Bu Cl H Cl t-Bu Cl H Cl t-Bu Cl F Cl Me Cl Br Br Me Cl Br Br Me Cl CF3 Br Et Cl Br Br Et CI Br Br Et Cl CF3 Br i-Pr CI Br Br i-Pr Cl Br Br i-Pr Cl CF3 Br t-Bu Cl Br Br t-Bu Cl Br Br t-Bu Cl CF3 Br Me Cl Br Cl Me Cl I Cl Me Cl CF3 Cl Et Cl Br CI Et CI I Cl Et Cl CF3 Cl i-Pr Cl Br Cl i-Pr Cl I Cl i-Pr Cl CF3 Cl t-Bu Cl Br Cl t-Bu Cl I Cl t-Bu Cl CF3 Cl Me Cl I Br Me Cl I Br Me Br F Cl Et Cl I Br Et Cl I Br Et Br F Cl i-Pr Cl I Br i-Pr Cl I Br i-Pr Br F Cl t-Bu Cl I Br t-Bu Cl I Br t-Bu Br F Cl Me Cl I Cl Me Cl CF3 Cl Me Br F Br Et Cl I Cl Et Cl CF3 Cl Et Br F Br i-Pr Cl I Cl i-Pr Cl CF3 Cl i-Pr Br F Br t-Bu Cl I Cl t-Bu Cl CF3 Cl t-Bu Br F Br Me Cl CF3 Br Me Cl CF3 Br Me Br Cl Cl Et Cl CF3 Br Et Cl CF3 Br Et Br Cl Cl i-Pr Cl CF3 Br i-Pr Cl CF3 Br i-Pr Br Cl Cl t-Bu Cl CF3 Br t-Bu Cl CF3 Br t-Bu Br Cl Cl Me Cl CF3 Cl n-Pr Cl Cl Cl Me Br Cl Br Et Cl CF3 Cl n-Bu Cl Cl Cl Et Br Cl Br i-Pr Cl CF3 Cl s-Bu Cl Cl Cl i-Pr Br Cl Br t-Bu Cl CF3 Cl i-Bu Cl Cl Cl t-Bu Br Cl Br Me Br F Cl Me Br F Cl Me Br Br Cl Et Br F Cl Et Br F Cl Et Br Br Cl i-Pr Br F Cl i-Pr Br F Cl i-Pr Br Br Cl t-Bu Br F Cl t-Bu Br F Cl t-Bu Br Br Cl Me Br F Br Me Br F Br Me Br Br Br R5 is CHF2 R5 is CH2CF3 R5 is CF2CHF2 R3 R4a R4b R6 R3 R4a R4b R6 R3 R4a R4b R6 Et Br F Br Et Br F Br Et Br Br Br i-Pr Br F Br i-Pr Br F Br i-Pr Br Br Br t-Bu Br F Br t-Bu Br F Br t-Bu Br Br Br Me Br Cl Cl Me Br Cl Cl Me Br I Cl Et Br Cl Cl Et Br Cl Ci Et Br I Cl i-Pr Br Cl Cl i-Pr Br Cl Cl i-Pr Br I Cl t-Bu Br Cl Cl t-Bu Br Cl Cl t-Bu Br I Cl Me Br Cl Br Me Br Cl Br Me Br I Br Et Br Cl Br Et Br Cl Br Et Br I Br i-Pr Br Cl Br i-Pr Br Cl Br i-Pr Br I Br t-Bu Br Cl Br t-Bu Br Cl Br t-Bu Br I Br Me Br Br Cl Me Br Br Cl Me Br CF3 Cl Et Br Br Cl Et Br Br Cl Et Br CF3 Cl i-Pr Br Br Cl i-Pr Br Br CI i-Pr Br CF3 Cl t-Bu Br Br Cl t-Bu Br Br Cl t-Bu Br CF3 CI Me Br Br Br Me Br Br Br Me Br CF3 Br Et Br Br Br Et Br Br Br Et Br CF3 Br i-Pr Br Br Br i-Pr Br Br Br i-Pr Br CF3 Br t-Bu Br Br Br t-Bu Br Br Br t-Bu Br CF3 Br Me Br I Cl Me Br I Cl Me Cl Cl Br Et Br I Cl Et Br I Cl Et Cl Cl Br i-Pr Br I Cl i-Pr Br I Cl i-Pr Cl Cl Br t-Bu Br I Cl t-Bu Br I Cl t-Bu Cl Cl Br Me Br I Br Me Br I Br Me Cl Cl Cl Et Br I Br Et Br I Br Et CI Cl CI i-Pr Br I Br i-Pr Br I Br i-Pr Cl Cl Cl t-Bu Br I Br t-Bu Br I Br t-Bu Cl Cl Cl Table 26 R5 is CHF2 R5 is CH2F3 R5 is CF2CHF2 R3 R4a R4b R6 R3 R4a R4b R6 R3 R4a R4b R6 Me CH3 H Cl Me CH3 H Cl Me CH3 Br Cl Et CH3 H Cl Et CH3 H Cl Et CH3 Br Cl i-Pr CH3 H Cl i-Pr CH3 H Cl i-Pr CH3 Br Cl t-Bu CH3 H Cl t-Bu CH3 H Cl t-Bu CH3 Br Cl Me CH3 H Br Me CH3 H Br Me CH3 Br Br Et CH3 H Br Et CH3 H Br Et CH3 Br Br i-Pr CH3 H Br i-Pr CH3 H Br i-Pr CH3 Br Br t-Bu CH3 H Br t-Bu CH3 H Br t-Bu CH3 Br Br Me CH3 F Cl Me CH3 Br Cl Me CH3 I Cl Et CH3 F Cl Et CH3 Br Cl Et CH3 I Cl i-Pr CH3 F CI i-Pr CH3 Br Cl i-Pr CH3 I Cl t-Bu CH3 F Cl t-Bu CH3 Br Cl t-Bu CH3 I Cl Me CH3 F Br Me CH3 Br Br Me CH3 I Br Et CH3 F Br Et CH3 Br Br Et CH3 I Br i-Pr CH3 F Br i-Pr CH3 Br Br i-Pr CH3 I Br t-Bu CH3 F Br t-Bu CH3 Br Br t-Bu CH3 I Br Me CH3 Cl Cl Me CH3 F Cl Me CH3 CF3 CI Et CH3 Cl Cl Et CH3 F Cl Et CH3 CF3 Cl i-Pr CH3 Cl Cl i-Pr CH3 F Cl i-Pr CH3 CF3 CI t-Bu CH3 Cl Cl t-Bu CH3 F Cl t-Bu CH3 CF3 Cl Me CH3 Cl Br Me CH3 F Br Me CH3 CF3 Br Et CH3 Cl Br Et CH3 F Br Et CH3 CF3 Br i-Pr CH3 Cl Br i-Pr CH3 F Br i-Pr CH3 CF3 Br t-Bu CH3 CI Br t-Bu CH3 F Br t-Bu CH3 CF3 Br Me CH3 Br Cl Me CH3 Cl Cl Me CH3 Cl Cl Et CH3 Br Cl Et CH3 Cl Cl Et CH3 Cl Cl i-Pr CH3 Br CI i-Pr CH3 Cl Cl i-Pr CH3 Cl Cl t-Bu CH3 Br Cl t-Bu CH3 Cl Cl t-Bu CH3 Cl Cl R5 is CHF2 R5 is CH2F3 R5 is CF2CHF2 R3 R4a R4b R6 R3 R4a R4b R6 R3 R4a R4b R6 Me CH3 Br Br Me CH3 CI Br Me CH3 Cl Br Et CH3 Br Br Et CH3 Cl Br Et CH3 Cl Br i-Pr CH3 Br Br i-Pr CH3 Cl Br i-Pr CH3 Cl Br t-Bu CH3 Br Br t-Bu CH3 Cl Br t-Bu CH3 Cl Br Me CH3 I Cl Me CH3 I Cl Me CH3 H Cl Et CH3 I Cl Et CH3 I Cl Et CH3 H Cl i-Pr CH3 I Cl i-Pr CH3 I Cl i-Pr CH3 H Cl t-Bu CH3 I CI t-Bu CH3 I Cl t-Bu CH3 H Cl Me CH3 I Br Me CH3 I Br Me CH3 H Br Et CH3 I Br Et CH3 I Br Et CH3 H Br i-Pr CH3 I Br i-Pr CH3 I Br i-Pr CH3 H Br t-Bu CH3 I Br t-Bu CH3 I Br t-Bu CH3 H Br Me CH3 CF3 Cl Me CH3 CF3 Cl Me CH3 F Cl Et CH3 CF3 Cl Et CH3 CF3 Cl Et CH3 F Cl i-Pr CH3 CF3 CI i-Pr CH3 CF3 Cl i-Pr CH3 F Cl t-Bu CH3 CF3 Cl t-Bu CH3 CF3 Cl t-Bu CH3 F Cl Me CH3 CF3 Br Me CH3 CF3 Br Me CH3 F Br Et CH3 CF3 Br Et CH3 CF3 Br Et CH3 F Br i-Pr CH3 CF3 Br i-Pr CH3 CF3 Br i-Pr CH3 F Br t-Bu CH3 CF3 Br t-Bu CH3 CF3 Br t-Bu CH3 F Br n-Pr CH3 Cl Cl Me Cl H Br Me Cl Cl Br n-Bu CH3 Cl Cl Et Cl H Br Et Cl Cl Br s-Bu CH3 Cl Cl i-Pr Cl H Br i-Pr Cl Cl Br i-Bu CH3 Cl Cl t-Bu CI H Br t-Bu Cl Cl Br Me Cl I Br Me Cl H Cl Me Cl CI Ci Et Cl I Br Et Cl H Cl Et Cl Cl Cl i-Pr Cl I Br i-Pr Cl H Cl i-Pr Cl Cl Cl t-Bu Cl I Br t-Bu Cl H Cl t-Bu Cl Cl CI Me Cl I Cl Me Cl Cl Br Me Cl I Br Et Cl I Cl Et Cl Cl Br Et Cl I Br i-Pr Cl I Cl i-Pr Cl Cl Br i-Pr CI I Br t-Bu Cl I CI t-Bu Cl Cl Br t-Bu Cl I Br Me Cl H Br Me Cl Cl Cl Me Cl I Cl Et Cl H Br Et Cl Cl Cl Et Cl I Cl i-Pr Cl H Br i-Pr Cl Cl CI i-Pr Cl I CI t-Bu Cl H Br t-Bu Cl Cl Cl t-Bu Cl I Cl R5 is CHF2 r5 is CH2F3 R5 is CF2CHF2 R3 R4a R4b R6 R3 R4a R4b R6 R3 R4a R4b R6 Me Cl H Cl Me Cl F Br Me CI F Br Et Cl H ci Et Cl F Br Et ci F Br i-Pr Cl H Cl i-Pr Cl F Br i-Pr Cl F Br t-Bu Cl H Cl t-Bu Cl F Br t-Bu Cl F Br Me Cl CF3 Br Me Cl F Cl Me Cl F Cl Et CI CF3 Br Et Cl F Cl Et Cl F Cl i-Pr Cl CF3 Br i-Pr Cl F Cl i-Pr Cl F Cl t-Bu Cl CF3 Br t-Bu Cl F Cl t-Bu Cl F Cl Me Cl CF3 Cl Me Cl Br Br Me Cl H Br Et Cl CF3 Cl Et Cl Br Br Et Cl H Br i-Pr Cl CF3 Cl i-Pr Cl Br Br i-Pr Cl H Br t-Bu Cl CF3 Cl t-Bu Cl Br Br t-Bu Cl H Br Me Cl Br Br Me CI I Cl Me Cl H Cl Et Cl Br Br Et Cl I Cl Et Cl H Cl i-Pr Cl Br Br i-Pr Cl I Cl i-Pr Cl H Cl t-Bu Cl Br Br t-Bu Cl I Cl i-Pr Cl H Cl Me Cl Br Cl Me Cl I Br Me Cl CF3 Br Et CI Br Cl Et Cl I Br Et Cl CF3 Br i-Pr Cl Br Cl i-Pr Cl I Br i-Pr Cl CF3 Br t-Bu Cl Br Cl t-Bu Cl I Br t-Bu Cl CF3 Br Me Cl F Br Me Cl CF3 Cl Me Cl CF3 Cl Et Cl F Br Et Cl CF3 Cl Et Cl CF3 Cl i-Pr Cl F Br i-Pr Cl CF3 Cl i-Pr Cl CF3 Cl t-Bu Cl F Br t-Bu Cl CF3 Cl t-Bu Cl CF3 Cl Me Cl Cl Cl Me Cl CF3 Br Me Br F Cl Et Cl Cl Cl Et Cl CF3 Br Et Br F Cl i-Pr Cl Cl CI i-Pr Cl CF3 Br i-Pr Br F Cl t-Bu Cl Cl Cl t-Bu Cl CF3 Br t-Bu Br F Cl Me Cl F Cl n-Pr Cl CI Cl Me Br F Br Et Cl F Cl n-Bu Cl Cl Cl Et Br F Br i-Pr Cl F Cl s-Bu Cl Cl Cl i-Pr Br F Br t-Bu Cl F Cl i-Bu Cl Cl Cl t-Bu Br F Br Me Br Br Cl Me Br F Cl Me Br CI Cl Et Br Br Cl Et Br F Cl Et Br Cl Cl i-Pr Br Br Cl i-Pr Br F Cl i-Pr Br Cl Cl t-Bu Br Br Cl t-Bu Br F Cl t-Bu Br Cl Cl R5 is CHF2 R5 is CHIEZ RS is CF2CHF2 R3 R4a R4b R6 R3 R4a R4b R6 R3 R4a R4b R6 Me Br Br Br Me Br F Br Me Br Cl Br Et Br Br Br Et Br F Br Et Br Cl Br i-Pr Br Br Br i-Pr Br F Br i-Pr Br Cl Br t-Bu Br Br Br t-Bu Br F Br t-Bu Br Cl Br Me Br I Cl Me Br Cl Cl Me Br Br Ci Et Br I Cl Et Br Cl CI Et Br Br ci i-Pr Br I Cl i-Pr Br CI Cl i-Pr Br Br Cl t-Bu Br I Cl t-Bu Br Cl Cl t-Bu Br Br CI Me Br I Br Me Br Cl Br Me Br Br Br Et Br I Br Et Br Cl Br Et Br Br Br i-Pr Br I Br i-Pr Br Cl Br i-Pr Br Br Br t-Bu Br I Br t-Bu Br Cl Br t-Bu Br Br Br Me Br F Cl Me Br I Cl Me Br CF3 Cl Et Br F ci Et Br I CI Et Br CF3 Cl i-Pr Br F Cl i-Pr Br I Cl i-Pr Br CF3 Cl t-Bu Br F CI t-Bu Br I Cl t-Bu Br CF3 Cl Me Br F Br Me Br I Br Me Br CF3 Br Et Br F Br Et Br I Br Et Br CF3 Br i-Pr Br F Br i-Pr Br I Br i-Pr Br CF3 Br t-Bu Br F Br t-Bu Br I Br t-Bu Br CF3 Br Me Br Cl Cl Me Br Br Cl Me Br I Cl Et Br Cl Cl Et Br Br Cl Et Br I ci i-Pr Br Cl Cl i-Pr Br Br Cl i-Pr Br I Cl t-Bu Br Cl Cl t-Bu Br Br Cl t-Bu Br I Cl Me Br Cl Br Me Br Br Br Me Br I Br Et Br Cl Br Et Br Br Br Et Br I Br i-Pr Br Cl Br i-Pr Br Br Br i-Pr Br I Br t-Bu Br Cl Br t-Bu Br Br Br t-Bu Br I Br Table 27 R5 is CHF2 r5 is CH2F3 R5 is CF2CHF2 R3 R4a R4b R6 R3 R4a R4b R6 R3 R4a R4b R6 Me CH3 H Cl Me CH3 H Cl Me CH3 Br Cl Et CH3 H Cl Et CH3 H CI Et CH3 Br Cl i-Pr CH3 H Cl i-Pr CH3 H Cl i-Pr CH3 Br Cl t-Bu CH3 H Cl t-Bu CH3 H Cl t-Bu CH3 Br CI Me CH3 H Br Me CH3 H Br Me CH3 Br Br Et CH3 H Br Et CH3 H Br Et CH3 Br Br i-Pr CH3 H Br i-Pr CH3 H Br i-Pr CH3 Br Br t-Bu CH3 H Br t-Bu CH3 H Br t-Bu CH3 Br Br Me CH3 F Cl Me CH3 Br Cl Me CH3 I Cl Et CH3 F Cl Et CH3 Br CI Et CH3 I Cl i-Pr CH3 F Cl i-Pr CH3 Br Cl i-Pr CH3 I Cl t-Bu CH3 F Cl t-Bu CH3 Br Cl t-Bu CH3 I CI Me CH3 F Br Me CH3 Br Br Me CH3 I Br Et CH3 F Br Et CH3 Br Br Et CH3 I Br i-Pr CH3 F Br i-Pr CH3 Br Br i-Pr CH3 I Br t-Bu CH3 F Br t-Bu CH3 Br Br t-Bu CH3 I Br Me CH3 Cl Cl Me CH3 F Cl Me CH3 CF3 Cl Et CH3 Cl Cl Et CH3 F Cl Et CH3 CF3 Cl i-Pr CH3 Cl Cl i-Pr CH3 F Cl i-Pr CH3 CF3 CI t-Bu CH3 CI Cl t-Bu CH3 F Cl t-Bu CH3 CF3 Cl Me CH3 Cl Br Me CH3 F Br Me CH3 CF3 Br Et CH3 Cl Br Et CH3 F Br Et CH3 CF3 Br i-Pr CH3 Cl Br i-Pr CH3 F Br i-Pr CH3 CF3 Br t-Bu CH3 CI Br t-Bu CH3 F Br t-Bu CH3 CF3 Br Me CH3 Br Cl Me CH3 Cl Cl Me CH3 Cl Cl Et CH3 Br Cl Et CH3 Cl Cl Et CH3 Cl CI i-Pr CH3 Br Cl i-Pr CH3 Cl Cl i-Pr CH3 Cl CI t-Bu CH3 Br Cl t-Bu CH3 Cl Cl t-Bu CH3 Cl Cl Me CH3 Br Br Me CH3 Cl Br Me CH3 Cl Br R5 is CHF2 r5 is CH2F3 R5 is CF2CHF2 R3 R4a R4b R6 R3 R4a R4b R6 R3 R4a R4b R6 Et CH3 Br Br Et CH3 Cl Br Et CH3 Cl Br i-Pr CH3 Br Br i-Pr CH3 Cl Br i-Pr CH3 Cl Br t-Bu CH3 Br Br t-Bu CH3 Cl Br t-Bu CH3 Cl Br Me CH3 I Cl Me CH3 I Cl Me CH3 H Cl Et CH3 I Ci Et CH3 I Cl Et CH3 H Cl i-Pr CH3 I Cl i-Pr CH3 I Cl i-Pr CH3 H Cl t-Bu CH3 I Cl t-Bu CH3 I Cl t-Bu CH3 H Cl Me CH3 I Br Me CH3 I Br Me CH3 H Br Et CH3 I Br Et CH3 I Br Et CH3 H Br i-Pr CH3 I Br i-Pr CH3 I Br i-Pr CH3 H Br t-Bu CH3 I Br t-Bu CH3 I Br t-Bu CH3 H Br Me CH3 CF3 Cl Me CH3 CF3 Cl Me CH3 F Cl Et CH3 CF3 Cl Et CH3 CF3 Cl Et CH3 F Cl i-Pr CH3 CF3 Cl i-Pr CH3 CF3 Cl i-Pr CH3 F Cl t-Bu CH3 CF3 Cl t-Bu CH3 CF3 CI t-Bu CH3 F Cl Me CH3 CF3 Br Me CH3 CF3 Br Me CH3 F Br Et CH3 CF3 Br Et CH3 CF3 Br Et CH3 F Br i-Pr CH3 CF3 Br i-Pr CH3 CF3 Br i-Pr CH3 F Br t-Bu CH3 CF3 Br t-Bu CH3 CF3 Br t-Bu CH3 F Br n-Pr CH3 Cl Cl Me Cl H Br Me Cl Cl Br -Bu CH3 Cl Cl Et Cl H Br Et Cl Cl Br s-Bu CH3 Cl Cl i-Pr Cl H Br i-Pr Cl Cl Br i-Bu CH3 Cl Cl t-Bu Cl H Br t-Bu CI Cl Br Me Cl I Br Me Cl H Cl Me Cl Cl Cl Et Cl I Br Et Cl H Cl Et Cl Cl Cl i-Pr Cl I Br i-Pr Cl H Cl i-Pr Cl Cl Cl t-Bu Cl I Br t-Bu Cl H Cl t-Bu Cl Cl Cl Me Cl I Cl Me Cl Cl Br Me Cl I Br Et Cl I Cl Et Cl Cl Br Et CI I Br i-Pr Cl I Cl i-Pr Cl Cl Br i-Pr Cl I Br t-Bu Cl I Cl t-Bu Cl Cl Br t-Bu Cl I Br Me Cl H Br Me Cl Cl Cl Me Cl I Ci Et Cl H Br Et Cl Cl Cl Et cl I Cl i-Pr Cl H Br i-Pr Cl Cl Cl i-Pr Cl I Cl t-Bu Cl H Br t-Bu Cl Cl Cl t-Bu Cl I Cl Me Cl H Cl Me Cl F Br Me Cl F Br R5 is CHF2 R5 is CH2F3 R5 is CF2CHF2 R3 R4a R4b R6 R3 R4a R4b R6 R3 R4a R4b R6 Et CI H Cl Et Cl F Br Et Cl F Br i-Pr Cl H Cl i-Pr Cl F Br i-Pr Cl F Br t-Bu Cl H Cl t-Bu Cl F Br t-Bu Cl F Br Me Cl CF3 Br Me Cl F Cl Me Cl F Cl Et ci CF3 Br Et Cl F Cl Et Cl F ci i-Pr Cl CF3 Br i-Pr Cl F Cl i-Pr Cl F Cl t-Bu Cl CF3 Br t-Bu Cl F Cl t-Bu Cl F Cl Me Cl CF3 Cl Me Cl Br Br Me Cl H Br Et Cl CF3 Cl Et Cl Br Br Et Cl H Br i-Pr Cl CF3 Cl i-Pr Cl Br Br i-Pr Cl H Br t-Bu CI CF3 Cl t-Bu Cl Br Br t-Bu Cl H Br Me Cl Br Br Me Cl I Cl Me Cl H CI Et Cl Br Br Et Cl I Cl Et Cl H Cl i-Pr Cl Br Br i-Pr Cl I Cl i-Pr Cl H Cl t-Bu Cl Br Br t-Bu Cl I Cl i-Pr Cl H CI Me CI Br Cl Me Cl I Br Me Cl CF3 Br Et Cl Br Cl Et Cl I Br Et Cl CF3 Br i-Pr Cl Br Cl i-Pr Cl I Br i-Pr Cl CF3 Br t-Bu Cl Br Cl t-Bu Cl I Br t-Bu Cl CF3 Br Me Cl F Br Me Cl CF3 Cl Me Cl CF3 Cl Et CI F Br Et Cl CF3 CI Et Cl CF3 Cl i-Pr Cl F Br i-Pr Cl CF3 Cl i-Pr Cl CF3 Cl t-Bu Cl F Br t-Bu Cl CF3 Cl t-Bu Cl CF3 Cl Me Cl Cl Cl Me Cl CF3 Br Me Br F Cl Et Cl Cl Cl Et Cl CF3 Br Et Br F CI i-Pr Cl Cl Cl i-Pr Cl CF3 Br i-Pr Br F Cl t-Bu Cl Cl Cl t-Bu Cl CF3 Br t-Bu Br F Cl Me Cl F Cl n-Pr Cl Cl Cl Me Br F Br Et Cl F Cl n-Bu Cl Cl Cl Et Br F Br i-Pr Cl F Cl s-Bu Cl Cl Cl i-Pr Br F Br t-Bu Cl F Cl i-Bu CI Cl Cl t-Bu Br F Br Me Br Br Cl Me Br F Cl Me Br Cl CI Et Br Br Cl Et Br F Cl Et Br Cl Cl i-Pr Br Br Cl i-Pr Br F Cl i-Pr Br Cl Cl t-Bu Br Br Cl t-Bu Br F Cl t-Bu Br Cl CI Me Br Br Br Me Br F Br Me Br Cl Br R5 is CH R5 is CH2F3 R5 is CF2CHF2 R3 R4a R4b R6 R3 R4a R4b R6 R3 R4a R4b R6 Et Br Br Br Et Br F Br Et Br Cl Br i-Pr Br Br Br i-Pr Br F Br i-Pr Br Cl Br t-Bu Br Br Br t-Bu Br F Br t-Bu Br Cl Br Me Br I Cl Me Br Cl Cl Me Br Br Cl Et Br I Cl Et Br Cl Cl Et Br Br Ci i-Pr Br I Cl i-Pr Br Cl Cl i-Pr Br Br Cl t-Bu Br I Cl t-Bu Br Cl Cl t-Bu Br Br Cl Me Br I Br Me Br Cl Br Me Br Br Br Et Br I Br Et Br Cl Br Et Br Br Br i-Pr Br I Br i-Pr Br Cl Br i-Pr Br Br Br t-Bu Br I Br t-Bu Br Cl Br t-Bu Br Br Br Me Br F Cl Me Br I Cl Me Br CF3 Cl Et Br F Cl Et Br I Cl Et Br CF3 Cl i-Pr Br F Cl i-Pr Br I Cl i-Pr Br CF3 Cl t-Bu Br F Cl t-Bu Br I Cl t-Bu Br CF3 Cl Me Br F Br Me Br I Br Me Br CF3 Br Et Br F Br Et Br I Br Et Br CF3 Br i-Pr Br F Br i-Pr Br I Br i-Pr Br CF3 Br t-Bu Br F Br t-Bu Br I Br t-Bu Br CF3 Br Me Br Cl Cl Me Br Br Cl Me Br I Cl Et Br Cl Cl Et Br Br Cl Et Br I Cl i-Pr Br Cl Cl i-Pr Br Br Cl i-Pr Br I Cl t-Bu Br Cl Cl t-Bu Br Br Cl t-Bu Br I Cl Me Br Cl Br Me Br Br Br Me Br I Br Et Br Cl Br Et Br Br Br Et Br I Br i-Pr Br Cl Br i-Pr Br Br Br i-Pr Br I Br t-Bu Br Cl Br t-Bu Br Br Br t-Bu Br I Br Table 28 R3 R4a R4b R5 R6 R3 R4a R4b R5 R6 R3 R4a R4b R5 R6 Me CH3 H CF3 Cl Me Cl H Cl Br Me Cl Br Cl Br Et CH3 H CF3 Cl Et Cl H Cl Br Et CI Br Cl Br i-Pr CH3 H CF3 Cl i-Pr Cl H Cl Br i-Pr Cl Br Cl Br t-Bu CH3 H CF3 Cl t-Bu Cl H Cl Br t-Bu Cl Br Cl Br Me CH3 H CF3 Br Me Cl H Br Cl Me Cl Br Br Cl Et CH3 H CF3 Br Et Cl H Br Cl Et Cl Br Br CI i-Pr CH3 H CF3 Br i-Pr Cl H Br Cl i-Pr Cl Br Br Cl t-Bu CH3 H CF3 Br t-Bu Cl H Br Cl t-Bu Cl Br Br Cl Me CH3 H Cl Cl Me Cl H Br Br Me Cl Br Br Br Et CH3 H Cl Cl Et Cl H Br Br Et Cl Br Br Br i-Pr CH3 H Cl Cl i-Pr CI H Br Br i-Pr Cl Br Br Br t-Bu CH3 H Cl Cl t-Bu Cl H Br Br t-Bu Cl Br Br Br Me CH3 H Cl Br Me Cl H CF3 Cl Me Cl I CF3 Cl Et CH3 H Cl Br Et Cl H CF3 Cl Et Cl I CF3 Cl i-Pr CH3 H Cl Br i-Pr Cl H CF3 Cl i-Pr Cl I CF3 Cl t-Bu CH3 H Cl Br t-Bu Cl H CF3 Cl t-Bu Cl I CF3 Cl Me CH3 H Br Cl Me Cl H CF3 Br Me Cl I CF3 Br Et CH3 H Br Cl Et Cl H CF3 Br Et Cl I CF3 Br i-Pr CH3 H Br Cl i-Pr Cl H CF3 Br i-Pr CI I CF3 Br t-Bu CH3 H Br Cl t-Bu Cl H CF3 Br t-Bu Cl I CF3 Br Me CH3 H Br Br Me Cl H Cl Cl Me Cl I Cl Cl Et CH3 H Br Br Et Cl H Cl CI Et Cl I Cl Cl i-Pr CH3 H Br Br i-Pr CI H Cl Cl i-Pr Cl I Cl Cl t-Bu CH3 H Br Br i-Pr Cl H Cl Cl t-Bu Cl I Cl Cl Me CH3 F CF3 Cl Me CH3 Cl CF3 Cl Me Cl I Cl Br Et CH3 F CF3 Cl Et CH3 Cl CF3 Cl Et CI I Cl Br i-Pr CH3 F CF3 Cl i-Pr CH3 Cl CF3 Cl i-Pr Cl I Cl Br t-Bu CH3 F CF3 Cl t-Bu CH3 Cl CF3 Cl t-Bu Cl I Cl Br Me CH3 F CF3 Br Me CH3 Cl CF3 Br Me Cl I Br Cl R3 R4a R4b R5 R6 R3 R4a R4b R5 R6 R3 R4a R4b R5 R6 Et CH3 F CF3 Br Et CH3 Cl CF3 Br Et Cl I Br Cl i-Pr CH3 F CF3 Br i-Pr CH3 Cl CF3 Br i-Pr Cl I Br CI t-Bu CH3 F CF3 Br t-Bu CH3 Cl CF3 Br t-Bu Cl I Br Cl Me CH3 F Cl Cl Me CH3 Cl Cl Cl Me Cl I Br Br Et CH3 F Cl Cl Et CH3 Cl Cl Cl Et CI I Br Br i-Pr CH3 F Cl Cl i-Pr CH3 Cl Cl Cl i-Pr Cl I Br Br t-Bu CH3 F Cl Cl t-Bu CH3 Cl Cl Cl t-Bu Cl I Br Br Me CH3 F Cl Br Me CH3 Cl Cl Br Me Cl CF3 CF3 Cl Et CH3 F Cl Br Et CH3 Cl Cl Br Et Cl CF3 CF3 Cl i-Pr CH3 F Cl Br i-Pr CH3 Cl Cl Br i-Pr Cl CF3 CF3 Cl t-Bu CH3 F Cl Br t-Bu CH3 Cl Cl Br t-Bu Cl CF3 CF3 Cl Me CH3 F Br Cl Me CH3 Cl Br Cl Me Cl CF3 CF3 Br Et CH3 F Br Cl Et CH3 Cl Br Cl Et Cl CF3 CF3 Br i-Pr CH3 F Br Cl i-Pr CH3 Cl Br Cl i-Pr Cl CF3 CF3 Br t-Bu CH3 F Br Cl t-Bu CH3 Cl Br Cl t-Bu Cl CF3 CF3'Br Me CH3 F Br Br Me CH3 Cl Br Br Me Cl CF3 Cl Cl Et CH3 F Br Br Et CH3 Cl Br Br Et Cl CF3 Cl Cl i-Pr CH3 F Br Br i-Pr CH3 Cl Br Br i-Pr Cl CF3 Cl Cl t-Bu CH3 F Br Br t-Bu CH3 Cl Br Br t-Bu Cl CF3 Cl Cl Me CH3 Br CF3 Cl Me Cl F CF3 Cl Me Cl CF3 Cl Br Et CH3 Br CF3 Cl Et Cl F CF3 Cl Et Cl CF3 Cl Br i-Pr CH3 Br CF3 Cl i-Pr Cl F CF3 Cl i-Pr Cl CF3 Cl Br t-Bu CH3 Br CF3 Cl t-Bu Cl F CF3 Cl t-Bu Cl CF3 Cl Br Me CH3 Br CF3 Br Me Cl F CF3 Br Me Cl CF3 Br Cl Et CH3 Br CF3 Br Et Cl F CF3 Br Et Cl CF3 Br Cl i-Pr CH3 Br CF3 Br i-Pr Cl F CF3 Br i-Pr Cl CF3 Br Cl t-Bu CH3 Br CF3 Br t-Bu Cl F CF3 Br t-Bu Cl CF3 Br Cl Me CH3 Br Cl Cl Me Cl F Cl Cl Me Cl CF3 Br Br Et CH3 Br Cl Cl Et Cl F Cl Cl Et Cl CF3 Br Br i-Pr CH3 Br Cl Cl i-Pr Cl F Cl Cl i-Pr Cl CF3 Br Br t-Bu CH3 Br Cl Cl t-Bu Cl F Cl Cl t-Bu Cl CF3 Br Br Me CH3 Br Cl Br Me Cl F Cl Br n-Pr Cl Cl Cl Cl Et CH3 Br Cl Br Et Cl F Cl Br n-Bu Cl Cl Cl Cl i-Pr CH3 Br Cl Br i-Pr Cl F Cl Br s-Bu Cl Cl Cl Cl t-Bu CH3 Br Cl Br t-Bu Cl F Cl Br i-Bu Cl Cl Cl Cl Me CH3 Br Br Cl Me Cl F Br Cl Me Br F CF3 Cl Et CH3 Br Br Cl Et Cl F Br Cl Et Br F CF3 Cl R3 R4a R4b R5 R6 R3 R4a R4b R5 R6 R3 R4a R4b R5 R6 i-Pr CH3 Br Br Cl i-Pr Cl F Br Cl i-Pr Br F CF3 Cl t-Bu CH3 Br Br Cl t-Bu Cl F Br Cl t-Bu Br F CF3 Cl Me CH3 Br Br Br Me Cl F Br Br Me Br F CF3 Br Et CH3 Br Br Br Et Cl F Br Br Et Br F CF3 Br i-Pr CH3 Br Br Br i-Pr Cl F Br Br i-Pr Br F CF3 Br t-Bu CH3 Br Br Br t-Bu Cl F Br Br t-Bu Br F CF3 Br Me CH3 I CF3 Cl Me Cl Cl CF3 Cl Me Br F Cl Cl Et CH3 I CF3 Cl Et Cl Cl CF3 Cl Et Br F Cl Cl i-Pr CH3 I CF3 Cl i-Pr Cl Cl CF3 Cl i-Pr Br F Cl Cl t-Bu CH3 I CF3 Cl t-Bu Cl Cl CF3 Cl t-Bu Br F Cl Cl Me CH3 I CF3 Br Me Cl Cl CF3 Br Me Br F Cl Br Et CH3 I CF3 Br Et Cl Cl CF3 Br Et Br F Cl Br i-Pr CH3 I CF3 Br i-Pr Cl Cl CF3 Br i-Pr Br F Cl Br t-Bu CH3 I CF3 Br t-Bu Cl Cl CF3 Br t-Bu Br F Cl Br Me CH3 I Cl Cl Me Cl Cl Cl Cl Me Br F Br Cl Et CH3 I Cl Cl Et CI Cl Cl Cl Et Br F Br Cl i-Pr CH3 I Cl Cl i-Pr Cl Cl Cl Cl i-Pr Br F Br Cl t-Bu CH3 I Cl Cl t-Bu Cl Cl Cl Cl t-Bu Br F Br Cl Me CH3 I Cl Br Me Cl Cl Cl Br Me Br F Br Br Et CH3 I Cl Br Et Cl Cl Cl Br Et Br F Br Br i-Pr CH3 I Cl Br i-Pr Cl Cl Cl Br i-Pr Br F Br Br t-Bu CH3 I Cl Br t-Bu Cl Cl Cl Br t-Bu Br F Br Br Me CH3 I Br Cl Me Br CF3 CF3 Cl Me Br Cl CF3 Cl Et CH3 I Br Cl Et Br CF3 CF3 Cl Et Br Cl CF3 Cl i-Pr CH3 I Br Cl i-Pr Br CF3 CF3 Cl i-Pr Br Cl CF3 Cl t-Bu CH3 I Br Cl t-Bu Br CF3 CF3 Cl t-Bu Br Cl CF3 Cl Me CH3 I Br Br Me Br CF3 CF3 Br Me Br Cl CF3 Br Et CH3 I Br Br Et Br CF3 CF3 Br Et Br Cl CF3 Br i-Pr CH3 I Br Br i-Pr Br CF3 CF3 Br i-Pr Br Cl CF3 Br t-Bu CH3 I Br Br t-Bu Br CF3 CF3 Br t-Bu Br Cl CF3 Br Me CH3 CF3 CF3 Cl Me Br CF3 Cl Cl Me Br Cl Cl Cl Et CH3 CF3 CF3 Cl Et Br CF3 Cl Cl Et Br Cl Cl Cl i-Pr CH3 CF3 CF3 Cl i-Pr Br CF3 Cl Cl i-Pr Br Cl Cl Cl t-Bu CH3 CF3 CF3 Cl t-Bu Br CF3 Cl Cl t-Bu Br Cl Cl Cl Me CH3 CF3 CF3 Br Me Br CF3 Cl Br Me Br Cl Cl Br Et CH3 CF3 CF3 Br Et Br CF3 Cl Br Et Br Cl Cl Br i-Pr CH3 CF3 CF3 Br i-Pr Br CF3 Cl Br i-Pr Br Cl Cl Br R3 R4a R4b R5 R6 R3 R4a R4b R5 R6 R3 R4a R4b R5 R6 t-Bu CH3 CF3 CF3 Br t-Bu Br CF3 Cl Br t-Bu Br Cl Cl Br Me CH3 CF3 Cl Cl Me Br CF3 Br Cl Me Br Cl Br Cl Et CH3 CF3 Cl Cl Et Br CF3 Br Cl Et Br Cl Br Cl i-Pr CH3 CF3 Cl Cl i-Pr Br CF3 Br Cl i-Pr Br Cl Br Cl t-Bu CH3 CF3 Cl Cl t-Bu Br CF3 Br Cl t-Bu Br Cl Br Cl Me CH3 CF3 Cl Br Me Br CF3 Br Br Me Br Cl Br Br Et CH3 CF3 Cl Br Et Br CF3 Br Br Et Br Cl Br Br i-Pr CH3 CF3 Cl Br i-Pr Br CF3 Br Br i-Pr Br Cl Br Br t-Bu CH3 CF3 Cl Br t-Bu Br CF3 Br Br t-Bu Br Cl Br Br Me CH3 CF3 Br Cl Me Br I CF3 Cl Me Br Br CF3 Cl Et CH3 CF3 Br Cl Et Br I CF3 Cl Et Br Br CF3 Cl i-Pr CH3 CF3 Br Cl i-Pr Br I CF3 Cl i-Pr Br Br CF3 Cl t-Bu CH3 CF3 Br Cl t-Bu Br I CF3 Cl t-Bu Br Br CF3 Cl Me CH3 CF3 Br Br Me Br I CF3 Br Me Br Br CF3 Br Et CH3 CF3 Br Br Et Br I CF3 Br Et Br Br CF3 Br i-Pr CH3 CF3 Br Br i-Pr Br I CF3 Br i-Pr Br Br CF3 Br t-Bu CH3 CF3 Br Br t-Bu Br I CF3 Br t-Bu Br Br CF3 Br n-Pr CH3 Cl Cl Cl Me Br I Cl Cl Me Br Br Cl Cl n-Bu CH3 Cl Cl Cl Et Br I Cl Cl Et Br Br Cl Cl s-Bu CH3 Cl Cl Cl i-Pr Br I Cl Cl i-Pr Br Br Cl Cl i-Bu CH3 Cl Cl Cl t-Bu Br I Cl Cl t-Bu Br Br Cl Cl Me Cl Cl Br Cl Me Br I Cl Br Me Br Br Cl Br Et Cl Cl Br Cl Et Br I Cl Br Et Br Br Cl Br i-Pr Cl Cl Br Cl i-Pr Br I Cl Br i-Pr Br Br Cl Br t-Bu Cl Cl Br Cl t-Bu Br I Cl Br t-Bu Br Br Cl Br Me Cl Cl Br Br Me Br I Br Cl Me Br Br Br Cl Et Cl Cl Br Br Et Br I Br Cl Et Br Br Br Cl i-Pr Cl Cl Br Br i-Pr Br I Br Cl i-Pr Br Br Br Cl t-Bu Cl Cl Br Br t-Bu Br I Br Cl t-Bu Br Br Br Cl Me Cl Br CF3 Cl Me Br I Br Br Me Br Br Br Br Et Cl Br CF3 Cl Et Br I Br Br Et Br Br Br Br i-Pr Cl Br CF3 Cl i-Pr Br I Br Br i-Pr Br Br Br Br t-Bu Cl Br CF3 Cl t-Bu Br I Br Br t-Bu Br Br Br Br Me Cl Br CF3 Br Me Cl Br Cl Cl t-Bu Cl Br CF3 Br Et Cl Br CF3 Br Et Cl Br Cl Cl t-Bu Cl Br Cl CI i-Pr Cl Br CF3 Br i-Pr Cl Br Cl Cl Table 29 R3 R4a R4b R5 R6 R3 R4a R4b R5 R6 R3 R4a R4b R5 R6 Me CH3 H CF3 Cl Me Cl F CF3 Cl Me Cl H Cl Br Et CH3 H CF3 Cl Et Cl F CF3 Cl Et Cl H Cl Br i-Pr CH3 H CF3 Cl -Pr Cl F CF3 Cl i-Pr Cl H Cl Br t-Bu CH3 H CF3 Cl t-Bu Cl F CF3 Cl t-Bu Cl H Cl Br Me CH3 H CF3 Br Me Cl F CF3 Br Me Cl H Br Cl Et CH3 H CF3 Br Et Cl F CF3 Br Et Cl H Br Cl i-Pr CH3 H CF3 Br i-Pr Cl F CF3 Br i-Pr Cl H Br Cl t-Bu CH3 H CF3 Br t-Bu Cl F CF3 Br t-Bu Cl H Br CI Me CH3 H Cl Cl Me Cl F Cl CI Me Cl H Br Br Et CH3 H Cl Cl Et Cl F Cl CI Et Cl H Br Br i-Pr CH3 H Cl Cl i-Pr Cl F Cl Cl i-Pr Cl H Br Br t-Bu CH3 H Cl Cl t-Bu Cl F Cl Cl t-Bu Cl H Br Br Me CH3 H Cl Br Me Cl F Cl Br Me Cl H CF3 Cl Et CH3 H Cl Br Et Cl F Cl Br Et Cl H CF3 Cl i-Pr CH3 H Cl Br i-Pr Cl F Cl Br i-Pr Cl H CF3 Cl t-Bu CH3 H Cl Br t-Bu Cl F Cl Br t-Bu Cl H CF3 Cl Me CH3 H Br Cl Me Cl F Br Cl Me Cl H CF3 Br Et CH3 H Br Cl Et Cl F Br Cl Et Cl H CF3 Br i-Pr CH3 H Br Cl i-Pr Cl F Br Cl i-Pr Cl H CF3 Br t-Bu CH3 H Br Cl t-Bu Cl F Br Cl t-Bu Cl H CF3 Br Me CH3 H Br Br Me Cl F Br Br Me Cl H Cl Cl Et CH3 H Br Br Et Cl F Br Br Et Cl H Cl Cl i-Pr CH3 H Br Br i-Pr Cl F Br Br i-Pr Cl H Cl Cl t-Bu CH3 H Br Br t-Bu Cl F Br Br i-Pr Cl H Cl Cl Me CH3 F CF3 Cl Me Cl Cl CF3 Cl Me Cl Br Cl Br Et CH3 F CF3 Cl Et Cl Cl CF3 Cl Et Cl Br Cl Br i-Pr CH3 F CF3 Cl i-Pr Cl Cl CF3 Cl i-Pr Cl Br Cl Br t-Bu CH3 F CF3 Cl t-Bu Cl Cl CF3 Cl t-Bu Cl Br Cl Br Me CH3 F CF3 Br Me Cl Cl CF3 Br Me Cl Br Br Cl R3 R4a R4b R5 R6 R3 R4a R4b R5 R6 R3 R4a R4b R5 R6 Et CH3 F CF3 Br Et Cl Cl CF3 Br Et Cl Br Br Cl i-Pr CH3 F CF3 Br i-Pr Cl Cl CF3 Br i-Pr Cl Br Br Cl t-Bu CH3 F CF3 Br t-Bu Cl Cl CF3 Br t-Bu Cl Br Br CI Me CH3 F Cl Cl Me Cl Cl Cl Cl Me Cl Br Br Br Et CH3 F Cl Cl Et Cl Cl Cl Cl Et Cl Br Br Br i-Pr CH3 F Cl Cl i-Pr Cl Cl Cl Cl i-Pr Cl Br Br Br t-Bu CH3 F Cl Cl t-Bu Cl Cl Cl Cl t-Bu Cl Br Br Br Me CH3 F Cl Br Me Cl Cl Cl Br Me Cl I CF3 Cl Et CH3 F Cl Br Et Cl Cl Cl Br Et Cl I CF3 Cl i-Pr CH3 F Cl Br i-Pr Cl Cl Cl Br i-Pr Cl I CF3 Cl t-Bu CH3 F Cl Br t-Bu Cl Cl Cl Br t-Bu Cl I CF3 Cl Me CH3 F Br Cl Me Cl Cl Br Cl Me Cl I CF3 Br Et CH3 F Br Cl Et Cl Cl Br Cl Et CI I CF3 Br i-Pr CH3 F Br Cl i-Pr Cl Cl Br Cl i-Pr Cl I CF3 Br t-Bu CH3 F Br Cl t-Bu Cl Cl Br Cl t-Bu Cl I CF3 Br Me CH3 F Br Br Me Cl Cl Br Br Me Cl I Cl CI Et CH3 F Br Br Et Cl Cl Br Br Et CI I Cl Cl i-Pr CH3 F Br Br i-Pr Cl Cl Br Br i-Pr Cl I Cl Cl t-Bu CH3 F Br Br t-Bu Cl Cl Br Br t-Bu Cl I Cl Cl Me CH3 Cl CF3 Cl Me Cl Br CF3 Cl Me Cl I Cl Br Et CH3 Cl CF3 Cl Et Cl Br CF3 Cl Et Cl I Cl Br i-Pr CH3 Cl CF3 Cl i-Pr Cl Br CF3 Cl i-Pr Cl I Cl Br t-Bu CH3 Cl CF3 Cl t-Bu Cl Br CF3 Cl t-Bu Cl I Cl Br Me CH3 Cl CF3 Br Me Cl Br CF3 Br Me Cl I Br Cl Et CH3 Cl CF3 Br Et CI Br CF3 Br Et Cl I Br Cl i-Pr CH3 Cl CF3 Br i-Pr Cl Br CF3 Br i-Pr Cl I Br Cl t-Bu CH3 Cl CF3 Br t-Bu Cl Br CF3 Br t-Bu Cl I Br Cl Me CH3 Cl Cl Cl Me Cl Br Cl Cl Me Cl I Br Br Et CH3 Cl Cl Cl Et Cl Br Cl Cl Et ci I Br Br i-Pr CH3 Cl Cl Cl i-Pr Cl Br Cl Cl i-Pr Cl I Br Br t-Bu CH3 Cl Cl Cl t-Bu Cl Br Cl Cl t-Bu Cl I Br Br Me CH3 Cl Cl Br Me Br Br Br Cl Me Cl CF3 CF3 Cl Et CH3 Cl Cl Br Et Br Br Br Cl Et Cl CF3 CF3 Cl i-Pr CH3 Cl Cl Br i-Pr Br Br Br Cl i-Pr Cl CF3 CF3 Cl t-Bu CH3 Cl Cl Br t-Bu Br Br Br Cl t-Bu Cl CF3 CF3 Cl Me CH3 Cl Br Cl Me Br Br Br Br Me Cl CF3 CF3 Br Et CH3 Cl Br Cl Et Br Br Br Br Et Cl CF3 CF3 Br R3 R4a R4b R5 R6 R3 R4a R4b R5 R6 R3 R4a R4b R5 R6 i-Pr CH3 Cl Br Cl i-Pr Br Br Br Br i-Pr Cl CF3 CF3 Br t-Bu CH3 Cl Br Cl t-Bu Br Br Br Br t-Bu Cl CF3 CF3 Br Me CH3 Cl Br Br Me Br I CF3 Cl Me Cl CF3 Cl Cl Et CH3 Cl Br Br Et Br I CF3 Cl Et Cl CF3 Cl Cl i-Pr CH3 Cl Br Br i-Pr Br I CF3 Cl i-Pr Cl CF3 Cl Cl t-Bu CH3 Cl Br Br t-Bu Br I CF3 Cl t-Bu Cl CF3 Cl Cl Me CH3 Br CF3 Cl Me Br I CF3 Br Me Cl CF3 Cl Br Et CH3 Br CF3 Cl Et Br I CF3 Br Et Cl CF3 Cl Br i-Pr CH3 Br CF3 Cl i-Pr Br I CF3 Br i-Pr Cl CF3 Cl Br t-Bu CH3 Br CF3 Cl t-Bu Br I CF3 Br t-Bu Cl CF3 Cl Br Me CH3 Br CF3 Br Me Br I Cl Cl Me Cl CF3 Br Cl Et CH3 Br CF3 Br Et Br I Cl Cl Et Cl CF3 Br Cl i-Pr CH3 Br CF3 Br i-Pr Br I Cl Cl i-Pr Cl CF3 Br Cl t-Bu CH3 Br CF3 Br t-Bu Br I Cl Cl t-Bu Cl CF3 Br Cl Me CH3 Br Cl Cl Me Br I Cl Br Me Cl CF3 Br Br Et CH3 Br Cl Cl Et Br I Cl Br Et Cl CF3 Br Br i-Pr CH3 Br Cl Cl i-Pr Br I Cl Br i-Pr Cl CF3 Br Br t-Bu CH3 Br Cl Cl t-Bu Br I Cl Br t-Bu Cl CF3 Br Br Me CH3 Br Cl Br Me Br I Br Cl n-Pr Cl Cl Cl Cl Et CH3 Br Cl Br Et Br I Br Cl n-Bu Cl Cl Cl CI i-Pr CH3 Br Cl Br i-Pr Br I Br Cl s-Bu Cl Cl Cl CI t-Bu CH3 Br Cl Br t-Bu Br I Br Cl i-Bu Cl Cl Cl CI Me CH3 Br Br Cl Me Br I Br Br Me Br F CF3 Cl Et CH3 Br Br Cl Et Br I Br Br Et Br F CF3 Cl i-Pr CH3 Br Br Cl i-Pr Br I Br Br i-Pr Br F CF3 Cl t-Bu CH3 Br Br Cl t-Bu Br I Br Br t-Bu Br F CF3 Cl Me CH3 Br Br Br Me Br CF3 CF3 Cl Me Br F CF3 Br Et CH3 Br Br Br Et Br CF3 CF3 Cl Et Br F CF3 Br i-Pr CH3 Br Br Br i-Pr Br CF3 CF3 Cl i-Pr Br F CF3 Br t-Bu CH3 Br Br Br t-Bu Br CF3 CF3 Cl t-Bu Br F CF3 Br Me CH3 I CF3 Cl Me Br CF3 CF3 Br Me Br F CI Cl Et CH3 I CF3 Cl Et Br CF3 CF3 Br Et Br F Cl Cl i-Pr CH3 I CF3 Cl i-Pr Br CF3 CF3 Br i-Pr Br F Cl Cl t-Bu CH3 I CF3 Cl t-Bu Br CF3 CF3 Br t-Bu Br F Cl Cl Me CH3 I CF3 Br Me Br CF3 Cl Cl Me Br F Cl Br Et CH3 I CF3 Br Et Br CF3 Cl Cl Et Br F Cl Br i-Pr CH3 I CF3 Br i-Pr Br CF3 Cl Cl i-Pr Br F Cl Br R3 R4a R4b R5 R6 R3 R4a R4b R5 R6 R3 R4a R4b R5 R6 t-Bu CH3 I CF3 Br t-Bu Br CF3 Cl Cl t-Bu Br F Cl Br Me CH3 I Cl Cl Me Br CF3 Cl Br Me Br F Br Cl Et CH3 I Cl Cl Et Br CF3 Cl Br Et Br F Br Cl i-Pr CH3 I Cl Cl i-Pr Br CF3 Cl Br i-Pr Br F Br Cl t-Bu CH3 I Cl Cl t-Bu Br CF3 Cl Br t-Bu Br F Br Cl Me CH3 I Cl Br Me Br CF3 Br Cl Me Br F Br Br Et CH3 I Cl Br Et Br CF3 Br Cl Et Br F Br Br i-Pr CH3 I Cl Br i-Pr Br CF3 Br Cl i-Pr Br F Br Br t-Bu CH3 I Cl Br t-Bu Br CF3 Br Cl t-Bu Br F Br Br Me CH3 I Br Cl Me Br CF3 Br Br Me Br Cl CF3 Cl Et CH3 I Br Cl Et Br CF3 Br Br Et Br Cl CF3 Cl i-Pr CH3 I Br Cl i-Pr Br CF3 Br Br i-Pr Br Cl CF3 Cl t-Bu CH3 I Br Cl t-Bu Br CF3 Br Br t-Bu Br Cl CF3 Cl Me CH3 I Br Br Me Br Br CF3 Cl Me Br Cl CF3 Br Et CH3 I Br Br Et Br Br CF3 Cl Et Br Cl CF3 Br i-Pr CH3 I Br Br i-Pr Br Br CF3 Cl i-Pr Br Cl CF3 Br t-Bu CH3 I Br Br t-Bu Br Br CF3 Cl t-Bu Br Cl CF3 Br Me CH3 CF3 CF3 Cl Me Br Br CF3 Br Me Br Cl Cl Cl Et CH3 CF3 CF3 Cl Et Br Br CF3 Br Et Br Cl Cl Cl i-Pr CH3 CF3 CF3 Cl i-Pr Br Br CF3 Br i-Pr Br Cl Cl Cl t-Bu CH3 CF3 CF3 Cl t-Bu Br Br CF3 Br t-Bu Br CI Cl Cl Me CH3 CF3 CF3 Br Me Br Br CI Cl Me Br Cl Cl Br Et CH3 CF3 CF3 Br Et Br Br Cl Cl Et Br Cl Cl Br i-Pr CH3 CF3 CF3 Br i-Pr Br Br Cl Cl i-Pr Br Cl Cl Br t-Bu CH3 CF3 CF3 Br t-Bu Br Br Cl Cl t-Bu Br Cl Cl Br Me CH3 CF3 Cl Cl Me Br Br Cl Br Me Br Cl Br Cl Et CH3 CF3 Cl Cl Et Br Br Cl Br Et Br Cl Br CI i-Pr CH3 CF3 Cl Cl i-Pr Br Br Cl Br i-Pr Br Cl Br Cl t-Bu CH3 CF3 Cl Cl t-Bu Br Br Cl Br t-Bu Br Cl Br Cl Me CH3 CF3 Cl Br Me CH3 CF3 Br Cl Me Br Cl Br Br Et CH3 CF3 Cl Br Et CH3 CF3 Br Cl Et Br Cl Br Br i-Pr CH3 CF3 Cl Br i-Pr CH3 CF3 Br Cl i-Pr Br Cl Br Br t-Bu CH3 CF3 Cl Br t-Bu CH3 CF3 Br Cl t-Bu Br Cl Br Br Me CH3 CF3 Br Br n-Pr CH3 Cl Cl Cl t-Bu CH3 CF3 Br Br Et CH3 CF3 Br Br zz-Bu CH3 Cl Cl Cl i-Bu CH3 Cl Cl Cl i-Pr CH3 CF3 Br Br s-Bu CH3 Cl Cl Cl Table 30 R4 R5a and/or R5b R4 R5a and/or R5b R4 R5a and/or R5b Me 2-CF3 Me 3-CF3 Me 4-CF3 Me 2-OCF3 Me 3-OCF3 Me 4-OCF3 Me 2-OCF2H Me 3-OCF2H Me 4-OCH Me 2-OCF2CF2H Me OCF2CF2H Me 4-OCF2CF2H Me 2-OCH2CF3 Me 3-OCH2CF3 Me 4-OCH2CF3 Me 2-SCF3 Me 3-SCF3 Me 4-SCF3 Me 2-SOCF3 Me 3-SOCF3 Me 4-SOCF3 Me 2-SO2CF3 Me 3-SOrCF3 Me 4-SOwCF3 Me 2-SCF2H Me 3-SCF2H Me 4-SCF-) H Me 2-SOCF2H Me 3-SOCF2H Me 4-SOCF2H Me 2-SO2CF2H Me 3-SO2CF2H Me 4-SO2CF2H Cl 2-CF3 Cl 3-CF3 CI 4-CF3 Cl 2-OCF3 Cl 3-OCF3 CI 4-OCF3 Cl 2-OCF2H Cl 3-OCF2H Cl 4-OCF2H Cl 2-OCF2CF2H Cl 3-OCF2CF2H Cl 4-OCF2CF2H Cl 2-OCH2CF3 Cl 3-OCH2CF3 Cl 4-OCH2CF3 Cl 2-SCF3 Cl 3-SCF3 Cl 4-SCF3 Cl 2-SOCF3 Cl 3-SOCF3 Cl 4-SOCF3 Cl 2-SOWCF3 Cl 3-SO2CF3 Cl 4-SO2CF3 Cl 2-SCF2H Cl 3-SCF2H Cl 4-SCF2H Cl 2-SOCF2H Cl 3-SOCF2H Cl 4-SOCF2H Cl 2-SO2CF2H Cl 3-SO2CF2H Cl 4-SO2CF2H F 2-CF3 F 3-CF3 F 4-CF3 F 2-OCF3 F 3-OCF3 F 4-OCF3 F 2-OCF2H F 3-OCF2H F 4-OCF2H F 2-OCF2CF2H F 3-OCF2CF2H F 4-OCF2CF2H F 2-OCH2CF3 F 3-OCHoCF3 F 4-OCH2CF3 F 2-SCF3 F 3-SCF3 F 4-SCF3 F 2-SOCF3 F 3-SOCF3 F 4-SOCF3 F 2-SO2CF3 F 3-SO2CF3 F 4-SO2CF3 F 2-SCF2H F 3-SCF2H F 4-SCF2H F 2-SOCF2H F 3-SOCFoH F 4-SOCF2H F 2-SO2CF2H F 3-SO2CF2H F 4-SO2CF2H Br 2-CF3 Br 3-CF3 Br 4-CF3 Br 2-OCF3 Br 3-OCF3 Br 4-OCF3 Br 2-OCFoH Br 3-OCF2H Br 4-OCF2H Br 2-OCF2CF2H Br 3-OCF2CF2H Br 4-OCF2CF2H Br 2-OCH2CF3 Br 3-OCH2CF3 Br 4-OCH2CF3 Br 2-SCF3 Br 3-SCF3 Br 4-SCF3 Br 2-SOCF3 Br 3-SOCF3 Br 4-SOCF3 Br 2-SO2CF3 Br 3-SO2CF3 Br 4-SO2CF3 Br 2-SCF2H Br 3-SCF2H Br 4-SCF2H Br 2-SOCF2H Br 3-SOCF2H Br 4-SOCF2H Br 2-SO2CF2H Br 3-SO2CF2H Br 4-SO2CF2H I 2-CF3 I 3-CF3 I 4-CF3 I 2-OCF3 I 3-OCF3 I 4-OCF3 I 2-OCF2H I 3-OCF2H I 4-OCF2H I 2-OCF2CF2H I 3-OCF2CF2H I 4-OCF2CF2H I 2-OCH2CF3 I 3-OCH2CF3 I 4-OCH2CF3 I 2-SCF3 I 3-SCF3 I 4-SCF3 I 2-SOCF3 I 3-SOCF3 I 4-SOCF3 I 2-SO2CF3 I 3-SO2CF3 I 4-SO2CF3 I 2-SCF2H I 3-SCFH I 4-SCF2H I 2-SOCF2H I 3-SOCF2H I 4-SOCF2H I 2-SO2CF2H I 3-SO2CF2H I 4-SO2CF2H OMe 2-CF3 OMe 3-CF3 OMe 4-CF3 OMe 2-OCF3 OMe 3-OCF3 OMe 4-OCF3 OMe 2-OCF2H OMe 3-OCFoH OMe 4-OCF2H OMe 2-OCF2CF2H OMe 3-OCF2CF2H OMe 4-OCF2CF2H OMe 2-OCH2CF3 OMe 3-OCH2CF3 OMe 4-OCH2CF3 OMe 2-SCF3 OMe 3-SCF3 OMe 4-SCF3 OMe 2-SOCF3 OMe 3-SOCF3 OMe 4-SOCF3 OMe 2-SO2CF3 OMe 3-SOoCF3 OMe 4-SO2CF3 OMe 2-SCF2H OMe 3-SCF2H OMe 4-SCF2H OMe 2-SOCF2H OMe 3-SOCF2H OMe 4-SOCF2H OMe 2-SO2CF2H OMe 3-SO2CF2H OMe 4-SO2CF2H CF3 2-CF3 CF3 3-CF3 CF3 4-CF3 CF3 2-OCF3 CF3 3-OCF3 CF3 4-OCF3 CF3 2-OCF2H CF3 3-OCFoH CF3 4-OCF2H CF3 2-OCF2CFoH CF3 3-OCF2CF2H CF3 4-OCFoCF2H CF3 2-OCH2CF3 CF3 3-OCH2CF3 CF3 4-OCH2CF3 CF3 2-SCF3 CF3 3-SCF3 CF3 4-SCF3 CF3 2-SOCF3 CF3 3-SOCF3 CF3 4-SOCF3 CF3 2-SO2CF3 CF3 3-SOoCF3 CF3 4-SO2CF3 CF3 2-SCF2H CF3 3-SCFoH CF3 4-SCF2H CF3 2-SOCF2H CF3 3-SOCF2H CF3 4-SOCF2H CF3 2-SO2CF2H CF3 3-SO2CF7H CF3 4-So2CF2H OCF2H 2-CF3 OCF2H 3-CF3 OCF2H 4-CF3 OCF2H 2-OCF3 OCF-) H 3-OCF3 OCFH 4-OCF3 OCF2H 2-OCF2H OCF2H 3-OCF2H OCF2H 4-OCFH OCF2H 2-OCFoCF2H OCF2H 3-OCF2CFH OCFH 4-OCFCFH OCF2H 2-OCH,) CF3 OCF2H 3-OCH2CF3 2 OCF2H 2-SCF3 OCF2H 3-SCF3 OCF2H 4-SCF3 OCF2H 2-SOCF3 OCF2H 3-SOCF3 OCF2H 4-SOCF3 OCFH 2-SO2CF3 OCF ? H 3-S02CF3 OCFH 4-S02CF3 OCF2H 2-SCF2H OCFH 3-SCF2H OCF2H 4-SCF2H OCFH 2-SOCF2H OCFH 3-SOCF2H OCFH 4-SOCF2H OCFH 2-SO2CF2H OCFH 3-SO2CF2H OCF2H 4-S02CFH Me 2-Me-4-CF3 F 2-Me-4-CF3 Me 2-Me-4-OCF3 F 2-Me-4-OCF3 Cl 2-Me-4-OCF3 Me 2-Me-4-OCF2H F 2-Me-4-OCF2H Cl 2-Me-4-OCF2H Me 2-Me-4-OCH2CF3 F 2-Me-4-OCHoCF3 Cl 2-Me-4-OCH2CF3 Me 2-Me-4-SCF3 F 2-Me-4-SCF3 Cl 2-Me-4-SCF3 Me 2-Me-4-SOCF3 F 2-Me-4-SOCF3 Cl 2-Me-4-SOCF3 Me 2-Me-4-SOaCF3 F 2-Me-4-S02CF3 Cl 2-Me-4-SO2CF3 Me 2-Me-4-SCFoH F 2-Me-4-SCFoH Cl 2-Me-4-SCF2H Me 2-Me-4-SOCF2H F 2-Me-4-SOCFoH Cl 2-Me-4-SOCF2H Me 2-Me-4-S02CF2H F 2-Me-4-SO2CF2H Cl 2-Me-4-SOrCFoH Br 2-Me-4-CF3 I 2-Me-4-CF3 OMe 2-Me-4-CF3 Br 2-Me-4-OCF3 I 2-Me-4-OCF3 OMe 2-Me-4-OCF3 Br 2-Me-4-OCF2H I 2-Me-4-OCF2H OMe 2-Me-4-OCF2H Br 2-Me-4-OCH2CF3 I 2-Me-4-OCH2CF3 OMe 2-Me-4-OCH2CF3 Br 2-Me-4-SCF3 I 2-Me-4-SCF3 OMe 2-Me-4-SCF3 Br 2-Me-4-SOCF3 I 2-Me-4-SOCF3 OMe 2-Me-4-SOCF3 Br 2-Me-4-SO2CF3 I 2-Me-4-SO2CF3 OMe 2-Me-4-SO2CF3

2-Me-4-SCF2H I 2-Me-4SCF2H OMe 2-Me-4-SCF2H 2-Me-4-SOCF2H I 2-Me-4-SOCF2H OMe 2-Me-4-SOCF2H 2-Me-4-SO2CF2H I 2-Me-4-SO2CF2H OMe 2-Me-4-SO2CF2H 2-Me-4-CF3 N02 2-Me-4-CF3 SMe 2-Me-4-CF3 2-Me-4-OCF3 No2 2-Me-4-OCF3 SMe 2-Me-4-OCF3 2-Me-4-OCF2H NO2 2-Me-4-OCF2H SMe 2-Me-4-OCF2H 2-Me-4-OCH2CF3 No2 2-Me-4-OCH2CF3 SMe 2-Me-4-OCH2CF3 2-Me-4-SCF3 N02 2-Me-4-SCF3 SMe 2-Me-4-SCF3 2-Me-4-SOCF3 No2 2-Me-4-SOCF3 SMe 2-Me-4-SOCF3 2-Me-4-SO2CF3 N02 2-Me-4-SO2CF3 SMe 2-Me-4-SO2CF3 2-Me-4-CF2H NO2 2-Me-4-SCF2H SMe 2-Me-4-SCF2H 2-Me-4-SOCF2H NO2 2-Me-4-SOCF2H SMe 2-Me-4-SOCF2H 2-Me-4-SO2CF2H NO2 2-Me-4-SO2CF2H SMe 2-Me-4-SO2CF2H Table 31 R5a and/or R5b R4 R5a and/or R5b R4 R5a and/or R5b 2-CF3 Me 3-CF3 Me 4-CF3 2-OCF3 Me 3-OCF3 Me 4-OCF3 2-OCF2H Me 3-OCFoH Me 4-OCF2H 2-OCF2CF2H Me 3-OCF2CF2H Me 4-OCF2CF2H 2-OCH2CF3 Me 3-OCH2CF3 Me 4-OCH2CF3 2-SCF3 Me 3-SCF3 Me 4-SCF3 2-SOCF3 Me 3-SOCF3 Me 4-SOCF3 2-SO2CF3 Me 3-SO2CF3 Me 4-SO2CF3 2-SCF2H Me 3-SCF2H Me 4-SCF2H 2-SOCF2H Me 3-SOCF2H Me 4-SOCF2H 2-SO2CF2H Me 3-SO2CF2H Me 4-SO2CF2H 2-CF3 Cl 3-CF3 Cl 4-CF3 2-OCF3 Cl 3-OCF3 Cl 4-OCF3 2-OCF2H Cl 3-OCF2H Cl 4-OCF2H 2-OCF2CF2H Cl 3-OCF2CF2H Cl 4-OCF2CF2H 2-OCHoCF3 Cl 3-OCH2CF3 Cl 4-OCH2CF3

2-SCF3 Cl 3-SCF3 Cl 4-SCF3 2-SOCF3 Cl 3-SOCF3 Cl 4-SOCF3 2-SO2CF3 Cl 3-S02CF3 Cl 4-S02CF3 2-SCF2H Cl 3-SCF2H Cl 4-SCF2H 2-SOCF2H Cl 3-SOCF2H Cl 4-SOCF2H 2-SO2CF2H Cl 3-SO2CF2H Cl 4-SO2CF2H 2-CF3 F 3-CF3 F 4-CF3 2-OCF3 F 3-OCF3 F 4-OCF3 2-OCF2H F 3-OCF2HY F 4-OCF2H 2-OCF2CF2H F 3-OCF2CF2H F 4-OCF2CF2H 2-OCH2CF3 F 3-OCH2CF3 F 4-OCH2CF3 2-SCF3 F 3-SCF3 F 4-SCF3 2-SOCF3 F 3-SOCF3 F 4-SOCF3 2-SO2CF3 F 3-SO2CF3 F 4-SO2CF3 2-SCF2H F 3-SCF2H F 4-SCF2H 2-SOCF2H F 3-SOCF2H F 4-SOCF2H 2-SO2CF2H F 3-SO2CF2H F 4-S02CF2H 2-CF3 Br 3-CF3 Br 4-CF3 2-OCF3 Br 3-OCF3 Br 4-OCF3 2-OCF2H Br 3-OCF2H Br 4-OCF2H 2-OCF2CF2H Br 3-OCF2CF2H Br 4-OCF2CF2H 2-OCH2CF3 Br 3-OCH2CF3 Br 4-OCH2CF3 2-SCF3 Br 3-SCF3 Br 4-SCF3 2-SOCF3 Br 3-SOCF3 Br 4-SOCF3 2-SO2CF3 Br 3-SO2CF3 Br 4-SO2CF3 2-SCF2H Br 3-SCF2H Br 4-SCF2H 2-SOCF2H Br 3-SOCF2H Br 4-SOCF2H 2-SO2CF2H Br 3-SO2CF2H Br 4-SO2CF2H 2-CF3 I 3-CF3 I 4-CF3 2-OCF3 I 3-OCF3 I 4-OCF3 2-OCF2H I 3-OCFH I 4-OCF2H 2-OCF2CF2H I 3-OCF2CF2H I 4-OCF2CF2H 2-OCH2CF3 I 3-OCH2CF3 I 4-OCH2CF3 2-SCF3 I 3-SCF3 I 4-SCF3 2-SOCF3 I 3-SOCF3 I 4-SOCF3 2-SO2CF3 I 3-SO2CF3 I 4-SOrCF3 2-SCF2H I 3-SCF2H I 4-SCF2H 2-SOCF2H I 3-SOCF2H I 4-SOCF2H I 2-SO2CF2H I 3-SO2CF2H I 4-SOCF2H OMe 2-CF3 OMe 3-CF3 OMe 4-CF3 OMe 2-OCF3 OMe 3-OCF3 OMe 4-OCF3 OMe 2-OCF2H OMe 3-OCF2H OMe 4-OCF2H OMe 2-OCF2CF2H OMe 3-OCF2CF2H OMe 4-OCF2CF2H OMe 2-OCHrCF3 OMe 3-OCH2CF3 OMe 4-OCH2CF3 OMe 2-SCF3 OMe 3-SCF3 OMe 4-SCF3 OMe 2-SOCF3 OMe 3-SOCF3 OMe 4-SOCF3 OMe 2-SO2CF3 OMe 3-SO2CF3 OMe 4-SO2CF3 OMe 2-SCF2H OMe 3-SCF2H OMe 4-SCF2H OMe 2-SOCF2H OMe 3-SOCF2H OMe 4-SOCF2H OMe 2-SO2CF2H OMe 3-SO2CF2H OMe 4-SO2CF2H CF3 2-CF3 CF3 3-CF3 CF3 4-CF3 CF3 2-OCF3 CF3 3-OCF3 CF3 4-OCF3 CF3 2-OCF2H CF3 3-OCF2H CF3 4-OCF2H CF3 2-OCF2CF2H CF3 3-OCF2CF2H CF3 4-OCF2CF2H CF3 2-OCH2CF3 CF3 3-OCH2CF3 CF3 4-OCH2CF3 CF3 2-SCF3 CF3 3-SCF3 CF3 4-SCF3 CF3 2-SOCF3 CF3 3-SOCF3 CF3 4-SOCF3 CF3 2-SOrCF3 CF3 3-SOnCF3 CF3 4-SOrCF3 CF3 2-SCF2H CF3 3-SCF2H CF3 4-SCF2H CF3 2-SOCF2H CF3 3-SOCF2H CF3 4-SOCF2H CF3 2-SO2CF2H CF3 3-SO2CF2H CF3 4-SO2CFH OCF2H 2-CF3 OCF2H 3-CF3 OCF2H 4-CF3 OCF2H 2-OCF3 OCF2H 3-OCF3 OCF2H 4-OCF3 OCF2H 2-OCF2H OCF2H 3-OCH2H OCF2H 4-OCF2H OCF2H 2-OCF2CF2H OCF2H 3-OCF2CF2H OCF2H 4-OCF2CF2H OCF2H 2-OCH2CF3 OCF2H 3-OCH2CF3 OCF2H 4-OCH2CF3 OCF2H 2-SCF3 OCF2H 3-SCF3 OCF2H 4-SCF3 OCF2H 2-SOCF3 OCF2H 3-SOCF3 OCF2H 4-SOCF3 OCF2H 2-SO2CF3 OCF2H 3-SO2CF3 OCF2H 4-SO2CF3 OCF2H 2-SCF2H OCF2H 3-SCF2H OCF2H 4-SCF2H OCF2H 2-SOCF2H OCF2H 3-SOCF2H OCF2H 4-SOCF2H OCF2H 2-S02CF2H OCF2H 3-SO2CF2H OCF2H 4-SO2CF2H Me 2-Me-4-CF3 F 2-Me-4-CF3 CI 2-Me-4-CF3 Me 2-Me-4-OCF3 F 2-Me-4-OCF3 Cl 2-Me-4-OCF3 Me 2-Me-4-OCF2H F 2-Me-4-OCF2H Cl 2-Me-4-OCF2H Me 2-Me-4-OCH2CF3 F 2-Me-4-OCH2CF3 Cl 2-Me-4-OCH2CF3

2-Me-4-SCF3 F 2-Me-4-SCF3 Cl 2-Me-4-SCF3 2-Me-4-SOCF3 F 2-Me-4-SOCF3 Cl 2-Me-4-SOCF3 2-Me-4-SO2CF3 F 2-Me-4-SO2CF3 Cl 2-Me-4-SO2CF3 2-Me-4-SCF2H F 2-Me-4-SCF2H Cl 2-Me-4-SCF2H 2-Me-4-SOCF2H F 2-Me-4-SOCF2H Cl 2-Me-4-SOCF2H 2-Me-4-SO2CF2H F 2-Me-4-SO2CF2H Cl 2-Me-4-SO2CF2H 2-Me-4-CF3 I 2-Me-4-CF3 OMe 2-Me-4-CF3 2-Me-4-OCF3 I 2-Me-4-OCF3 OMe 2-Me-4-OCF3 2-Me-4-OCF2H I 2-Me-4-OCF2H OMe 2-Me-4-OCF2H 2-Me-4-OCH2CF3 I 2-Me-4-OCH2CF3 OMe 2-Me-4-OCH2CF3 2-Me-4-SCF3 I 2-Me-4-SCF3 OMe 2-Me-4-SCF3 2-Me-4-SOCF3 I 2-Me-4-SOCF3 OMe 2-Me-4-SOCF3 2-Me-4-SO2CF3 I 2-Me-4-SO2CF3 OMe 2-Me-4-SO2CF3 2-Me-4-SCF2H I 2-Me-4-SCF2H OMe 2-Me-4-SCF2H 2-Me-4-SOCF2H I 2-Me-4-SOCF2H OMe 2-Me-4-SOCF2H 2-Me-4-S02CF2H I 2-Me-4-SO2CF2H OMe 2-Me-4-SO2CF2H 2-Me-4-CF3 N02 2-Me-4-CF3 SMe 2-Me-4-CF3 2-Me-4-OCF3 No2 2-Me-4-OCF3 SMe 2-Me-4-OCF3 2-Me-4-OCF2H NO2 2-Me-4-OCF2H SMe 2-Me-4-OCF2H 2-Me-4-OCH2CF3 No2 2-Me-4-OCH2CF3 SMe 2-Me-4-OCH2CF3 2-Me-4-SCF3 No2 2-Me-4-SCF3 SMe 2-Me-4-SCF3 2-Me-4-SOCF3 N02 2-Me-4-SOCF3 SMe 2-Me-4-SOCF3 2-Me-4-SO2CF3 NO2 2-Me-4-SO2CF3 SMe 2-Me-4-SO2CF3 2-Me-4-SCF2H NO2 2-Me-4-SCF2H SMe 2-Me-4-SCF2H 2-Me-4-SOCF2H No2 2-Me-4-SOCF2H SMe 2-Me-4-SOCF2H 2-Me-4-SO2CF2H NO2 2-Me-4-SO2CF2H SMe 2-Me-4-SO2CF2H Table 32 R5a and/or R5b R4 R5a and/or R5b R4 R5a and/or R5b 2-CF3 Me 3-CF3 Me 4-CF3 2-OCF3 Me 3-OCF3 Me 4-OCF3 2-OCF2H Me 3-OCF2H Me 4-OCF2H

2-OCF2CF2H Me 3-OCF2CF2H Me 4-OCF2CF2H 2-OCH2CF3 Me 3-OCH2CF3 Me 4-OCH2CF3 2-SCF3 Me 3-SCF3 Me 4-SCF3 2-SOCF3 Me 3-SOCF3 Me 4-SOCF3 2-SO2CF3 Me 3-SO2CF3 Me 4-SO2CF3 2-SCF2H Me 3-SCF2H Me 4-SCF ? H 2-SOCF2H Me 3-SOCF2H Me 4-SOCF2H 2-SO2CF2H Me 3-S02CF2H Me 4-SO2CF2H 2-CF3 Cl 3-CF3 Cl 4-CF3 2-OCF3 Cl 3-OCF3 Cl 4-OCF3 2-OCF2H Cl 3-OCF2H Cl 4-OCF2H 2-OCF2CF2H Cl 3-OCF2CF2H Cl 4-OCF2CF2H 2-OCH2CF3 Cl 3-OCH2CF3 CL 4-OCH2CF3 2-SCF3 Cl 3-SCF3 Cl 4-SCF3 2-SOCF3 Cl 3-SOCF3 Cl 4-SOCF3 2-SO2CF3 Cl 3-SO2VD3 Cl 4-SO2CF3 2-SCF2H Cl 3-SCF2H Cl 4-SCF2H 2-SOCF2H Cl 3-SOCF2H Cl 4-SOCF2H 2-SO2CF2H Cl 3-SO2CF2H Cl 4-SO2CF2H 2-CF3 F 3-CF3 F 4-CF3 2-OCF3 F 3-OCF3 F 4-OCF3 2-OCF2H F 3-OCFoH F 4-OCF2H 2-OCF2CF2H F 3-OCF2CF2H F 4-OCF2CF2H 2-OCH2CF3 F 3-OCH2CF3 F 4-OCH2CF3 2-SCF3 F 3-SCF3 F 4-SCF3 2-SOCF3 F 3-SOCF3 F 4-SOCF3 2-SO2CF3 F 3-SO2CF3 F 4-SO2CF3 2-SCF2H F 3-SCF2H F 4-SCF2H 2-SOCF2H F 3-SOCF2H F 4-SOCF2H 2-SO2CF2H F 3-SO2CF2H F 4-SO2CF2H 2-CF3 Br 3-CF3 Br 4-CF3 2-OCF3 Br 3-OCF3 Br 4-OCF3 2-OCF2H Br 3-OCF2H Br 4-OCF2H 2-OCF2CF2H Br 3-OCF2CF2H Br 4-OCF2CF2H 2-OCH2CF3 Br 3-OCH2CF3 Br 4-OCH2CF3 2-SCF3 Br 3-SCF3 Br 4-SCF3 2-SOCF3 Br 3-SOCF3 Br 4-SOCF3 2-SO2CF3 Br 3-SO2CF3 Br 4-SO2CF3 Br 2-SCF2H Br 3-SCF2H Br 4-SCF2H Br 2-SOCF2H Br 3-SOCF2H Br 4-SOCF2H Br 2-SO2CF2H Br 3-SO2CF2H Br 4-SO2CF2H I 2-CF3 I 3-CF3 I 4-CF3 I 2-OCF3 I 3-OCF3 I 4-OCF3 I 2-OCF2H I 3-OCF2H I 4-OCF2H I 2-OCF2CF2H I 3-OCF2CF2H I 4-OCF2CF2H I 2-OCH2CF3 I 3-OCH2CF3 I 4-OCH2CF3 I 2-SCF3 I 3-SCF3 I 4-SCF3 I 2-SOCF3 I 3-SOCF3 I 4-SOCF3 I 2-SO2CF3 I 3-SO2CF3 I 4-SO2CF3 I 2-SCF2H I 3-CF2H I 4-SCF2H I 2-SOCF2H I 3-SOCF2H I 4-SOCF2H I 2-SO2CF2H I 3-SO2CF2H I 4-SO2CF2H OMe 2-CF3 OMe 3-CF3 OMe 4-CF3 OMe 2-OCF3 OMe 3-OCF3 OMe 4-OCF3 OMe 2-OCF2H OMe 3-OCF2H OMe 4-OCF2H OMe 2-OCF2CF2H OMe 3-OCF2CF2H OMe 4-OCF2CF2H OMe 2-OCH2CF3 OMe 3-OCH2CF3 OMe 4-OCH2CF3 OMe 2-SCF3 OMe 3-SCF3 OMe 4-SCF3 OMe 2-SOCF3 OMe 3-SOCF3 OMe 4-SOCF3 OMe 2-SO2CF3 OMe 3-SO2CF3 OMe 4-SO2CF3 OMe 2-SCF2H OMe 3-SCF2H OMe 4-SCF2H OMe 2-SOCF2H OMe 3-SOCF2H OMe 4-SOCF2H OMe 2-SO2CF2H OMe 3-SO2CF2H OMe 4-SO2CF2H CF3 2-CF3 CF3 3-CF3 CF3 4-CF3 CF3 2-OCF3 CF3 3-OCF3 CF3 4-OCF3 CF3 2-OCF2H CF3 3-OCF2H CF3 4-OCFoH CF3 2-OCF2CF2H CF3 3-OCF2CF2H CF3 4-OCF2CF2H CF3 2-OCHvCF3 CF3 3-OCH2CF3 CF3 4-OCH2CF3 CF3 2-SCF3 CF3 3-SCF3 CF3 4-SCF3 CF3 2-SOCF3 CF3 3-SOCF3 CF3 4-SOCF3 CF3 2-SO2CF3 CF3 3-SO2CF3 CF3 4-SO2CF3 CF3 2-SCF2H CF3 3-SCF2H CF3 4-SCF2H CF3 2-SOCF2H CF3 3-SOCF2H CF3 4-SOCF2H CF3 2-SO2CF2H CF3 3-SO2CF2H CF3 4-SO2CF2H OCF2H 2-CF3 OCF2H 3-CF3 OCF2H 4-CF3 OCF2H 2-OCF3 OCF2H 3-OCF3 OCF2H 4-OCF3 OCF2H 2-OCF2H OCF2H 3-OCF2H OCF2H 4-OCF2H OCF2H 2-OCF2CF2H OCF2H 3-OCF2CF2H OCF2H 4-OCF2CF2H OCF2H 2-OCH2CF3 OCF2H 3-OCH2C3 OCF2H 4-OCH2CF3 OCF2H 2-SCF3 OCF2H 3-SCF3 OCF2H 4-SCF3 OCF2H 2-SOCF3 OCF2H 3-SOCF3 OCF2H 4-SOCF3 OCF2H 2-SO2CF3 OCF2H 3-SO2CF3 OCF2H 4-SO2CF3 OCF2H 2-SCF2H OCF2H 3-SCF2H OCF2H 4-SCF2H OCF2H 2-SOCF2H OCF2H 3-SOCF2H OCF2H 4-SOCF2H OCF2H 2-SO2CF2H OCF2H 3-SO2CF2H OCF2H 4-SO2CF2H Me 2-Me-4-CF3 F 2-Me-4-CF3 Cl 2-Me-4-CF3 Me 2-Me-4-OCF3 F 2-Me-4-OCF3 Cl 2-Me-4-OCF3 Me 2-Me-4-OCF2H F 2-Me-4-OCF2H Cl 2-Me-4-OCF2H Me 2-Me-4-OCH2CF3 F 2-Me-4-OCH2CF3 Cl 2-Me-4-OCH2CF3 Me 2-Me-4-SCF3 F 2-Me-4-SCF3 CI 2-Me-4-SCF3 Me 2-Me-4-SOCF3 F 2-Me-4-SOCF3 Cl 2-Me-4-SOCF3 Me 2-Me-4-SO2CF3 F 2-Me-4-SO2CF3 Cl 2-Me-4-SO2CF3 Me 2-Me-4-SCF2H F 2-Me-4-SCF2H Cl 2-Me-4-SCF2H Me 2-Me-4-SOCF2H F 2-Me-4-SOCF2H Cl 2-Me-4-SOCF2H Me 2-Me-4-SO2CF2H F 2-Me-4-SO2CF2H Cl 2-Me-4-SO2CF2H Br 2-Me-4-CF3 I 2-Me-4-CF3 OMe 2-Me-4-CF3 Br 2-Me-4-OCF3 I 2-Me-4-OCF3 OMe 2-Me-4-OCF3 Br 2-Me-4-OCF2H I 2-Me-4-OCF2H OMe 2-Me-4-OCF2H Br 2-Me-4-OCH2CF3 I 2-Me-4-OCH2CF3 OMe 2-Me-4-OCH2CF3 Br 2-Me-4-SCF3 I 2-Me-4-SCF3 OMe 2-Me-4-SCF3 Br 2-Me-4-SOCF3 I 2-Me-4-SOCF3 OMe 2-Me-4-SOCF3 Br 2-Me-4-SO2CF3 I 2-Me-4-SO2CF3 OMe 2-Me-4-SO2CF3 Br 2-Me-4-SCF2H I 2-Me-4-SCF2H OMe 2-Me-4-SCF2H Br 2-Me-4-SOCF2H I 2-Me-4-SOCF2H OMe 2-Me-4-SOCF2H Br 2-Me-4-SO2CF2H I 2-Me-4-SO2CF2H OMe 2-Me-4-SO2CF2H CF3 2-Me-4-CF3 No2 2-Me-4-CF3 SMe 2-Me-4-CF3 CF3 2-Me-4-OCF3 NOr 2-Me-4-OCF3 SMe 2-Me-4-OCF3 CF3 2-Me-4-OCF2H No2 2-Me-4-OCF2H SMe 2-Me-4-OCF2H CF3 2-Me-4-OCH2CF3 NO2 2-Me-4-OCH2CF3 SMe 2-Me-4-OCH2CF3 CF3 2-Me-4-SCF3 No2 2-Me-4-SCF3 SMe 2-Me-4-SCF3 CF3 2-Me-4-SOCF3 No2 2-Me-4-SOCF3 SMe 2-Me-4-SOCF3 CF3 2-Me-4-SO2CF3 No2 2-Me-4-SO2CF3 SMe 2-Me-4-SO2CF3 CF3 2-Me-4-SCF2H No2 2-Me-4-SCF2H SMe 2-Me-4-SCF2H CF3 2-Me-4-SOCF2H NO2 2-Me-4-SOCF2H SMe 2-Me-4-SOCF2H

2-Me-4-SO2CF2H NO2 2-Me-4-SO2CF2H SMe 2-Me-4-SO2CF2H Table 33 R5a and/or R5b R4 R5a and/or R5b R4 R5a and/or R5b 2-CF3 Me 3-CF3 Me 4-CF3 2-OCF3 Me 3-OCF3 Me 4-OCF3 2-OCF2H Me 3-OCF2H Me 4-OCF2H 2-OCF2CF2H Me 3-OCF2CF2H Me 4-OCF2CF2H 2-OCH2CF3 Me 3-OCH2CF3 Me 4-OCH2CF3 2-SCF3 Me 3-SCF3 Me 4-SCF3 2-SOCF3 Me 3-SOCF3 Me 4-SOCF3 2-SO2CF3 Me 3-SO2CF3 Me 4-SO2CF3 2-SCF2H Me 3-SCF2H Me 4-SCF2H 2-SOCF2H Me 3-SOCF2H Me 4-SOCF2H 2-SO2CF2H Me 3-SO2CF2H Me 4-SO2CF2H 2-CF3 Cl 3-CF3 Cl 4-CF3 2-OCF3 Cl 3-OCF3 Cl 4-OCF3 2-OCF2H Cl 3-OCF2H Cl 4-OCF2H 2-OCF2CF2H Cl 3-OCF2CF2H Cl 4-OCF2CF2H 2-OCH2CF3 Cl 3-OCH2CF3 Cl 4-OCH2CF3 2-SCF3 Cl 3-SCF3 Cl 4-SCF3 2-SOCF3 Cl 3-SOCF3 Cl 4-SOCF3 2-SO2CF3 Cl 3-SO2CF3 Cl 4-SO2CF3 2-SCF2H Cl 3-SCF2H Cl 4-SCF2H 2-SOCF2H Cl 3-SOCF2H Cl 4-SOCF2H 2-SO2CF2H Cl 3-SO2CF2H Cl 4-SO2CF2H 2-CF3 F 3-CF3 F 4-CF3 2-OCF3 F 3-OCF3 F 4-OCF3 2-OCF2H F 3-OCF2H F 4-OCF2H 2-OCF2CF2H F 3-OCF2CF2H F 4-OCF2CF2H 2-OCH2CF3 F 3-OCH2CF3 F 4-OCH2CF3 2-SCF3 F 3-SCF3 F 4-SCF3

2-SOCF3 F 3-SOCF3 F 4-SOCF3 2-SO2CF3 F 3-SO2CFR3 F 4-SO2CF3 2-SCV2H F 3-SCF2H F 4-SCF2H 2-SOCF2H F 3-SOCF2H F 4-SOCF2H 2-SO2CF2H F 3-SO2CF2H F 4-S02CF2H 2-CF3 Br 3-CF3 Br 4-CF3 2-OCF3 Br 3-OCF3 Br 4-OCF3 2-OCF2H Br 3-OCF2H Br 4-OCF2H 2-OCF2CF2H Br 3-OCF2CF2H Br 4-OCF2CF2H 2-OCH2CF3 Br 3-OCH2CF3 Br 4-OCH2CF3 2-SCF3 Br 3-SCF3 Br 4-SCF3 2-SOCF3 Br 3-SOCF3 Br 4-SOCF3 2-SO2CF3 Br 3-SO2CF3 Br 4-SO2CF3 2-SCF2H Br 3-SCF2H Br 4-SCF2H 2-SOCF2H Br 3-SOCF2H Br 4-SOCF2H 2-SO2CF2H Br 3-SO2CF2H Br 4-SO2CF2H 2-CF3 I 3-CF3 I 4-CF3 2-OCF3 I 3-OCF3 I 4-OCF3 2-OCF2H I 3-OCF2H I 4-OCF2H 2-OCF2CF2H I 3-OCF2CF2H I 4-OCF2CF2H 2-OCH2CF3 I 3-OCH2CF3 I 4-OCH2CF3 2-SCF3 I 3-SCF3 I 4-SCF3 2-SOCF3 I 3-SOCF3 I 4-SOCF3 2-SO2CF3 I 3-SO2CF3 I 4-SO2CF3 2-SCF2H I 3-SCF2H I 4-SCF2H 2-SOCF2H I 3-SOCF2H I 4-SOCF2H 2-SO2CF2H I 3-SO2CF2H I 4-SO2CF2H 2-CF3 OMe 3-CF3 OMe 4-CF3 2-OCF3 OMe 3-OCF3 OMe 4-OCF3 2-OCF2H OMe 3-OCF2H OMe 4-OCF2H 2-OCF2CF2H OMe 3-OCF2CF2H OMe 4-OCF2CF2H 2-OCH2CF3 OMe 3-OCH2CF3 OMe 4-OCH2CF3 2-SCF3 OMe 3-SCF3 OMe 4-SCF3 2-SOCF3 OMe 3-SOCF3 OMe 4-SOCF3 2-SO2CF3 OMe 3-SO2CF3 OMe 4-SO2CF3 2-SCF2H OMe 3-SCF2H OMe 4-SCF2H 2-SOCF2H OMe 3-SOCF2H OMe 4-SOCF2H 2-SO2CF2H OMe 3-SO2CF2H OMe 4-SO2CF2H CF3 2-CF3 CF3 3-CF3 CF3 4-CF3 CF3 2-OCF3 CF3 3-OCF3 CF3 4-OCF3 CF3 2-OCF2H CF3 3-OCF2H CF3 4-OCF2H CF3 2-OCF2CF2H CF3 3-OCF2CF2H CF3 4-OCF2CF2H CF3 2-OCH2CF3 CF3 3-OCH2CF3 CF3 4-OCH2CF3 CF3 2-SCF3 CF3 3-SCF3 CF3 4-SCF3 CF3 2-SOCF3 CF3 3-SOCF3 CF3 4-SOCF3 CF3 2-SO2CF3 CF3 3-SO2CF3 CF3 4-SO2CF3 CF3 2-SCF2H CF3 3-SCF2H CF34-SCF2H CF3 2-SOCF2H CF3 3-SOCF2H CF3 4-SOCF2H CF3 2-SO2CF2H CF3 3-S02CF2H CF3 4-S02CF2H OCF2H 2-CF3 OCF2H 3-CF3 OCF2H 4-CF3 OCF2H 2-OCF3 OCF2H 3-OCF3 OCF2H 4-OCF3 OCF2H 2-OCF2H OCF2H 3-OCF2H OCF2H 4-OCF2H OCF2H 2-OCF2CF2H OCF2H 3-OCF2CF2H OCF2H 4-OCF2CF2H OCF2H 2-OCH2CF3 OCF2H 3-OCH2CF3 OCF2H 4-OCH2CF3 OCF2H 2-SCF3 OCF2H 3-SCF3 OCF2H 4-SCF3 OCF2H 2-SOCF3 OCF2H 3-SOCF3 OCF2H 4-SOCF3 OCF2H 2-SO2CF2 OCF2H 3-SO2CF3 OCF2H 4-SO2CF3 OCF2H 2-SCF2H OCF2H 3-SCF2H OCF2H 4-SCF2H OCF2H 2-SOCF2H OCF2H 3-SOCF2H OCF2H 4-SOCF2H OCF2H 2-SO2CF2H OCF2H 3-SO2CF2H OCF2H 4-SO2CF2H Me 2-Me-4-CF3 F 2-Me-4-CF3 Cl 2-Me-4-CF3 Me 2-Me-4-OCF3 F 2-Me-4-OCF3 Cl 2-Me-4-OCF3 Me 2-Me-4-OCF2H F 2-Me-4-OCF2H Cl 2-Me-4-OCF2H Me 2-Me-4-OCH2CF3 F 2-Me-4-OCH2CF3 Cl 2-Me-4-OCH2CF3 Me 2-Me-4-SCF3 F 2-Me-4-SCF3 Cl 2-Me-4-SCF3 Me 2-Me-4-SOCF3 F 2-Me-4-SOCF3 Cl 2-Me-4-SOCF3 Me 2-Me-4-SO2CF3 F 2-Me-4-SO2CF3 Cl 2-Me-4-SO2CF3 Me 2-Me-4-SCF2H F 2-Me-4-SCF2H Cl 2-Me-4-SCF2H Me 2-Me-4-SOCF2H F 2-Me-4-SOCF2H Cl 2-Me-4-SOCF2H Me 2-Me-4-SO2CF2H F 2-Me-4-SO2CF2H Cl 2-Me-4-SO2CF2H Br 2-Me-4-CF3 I 2-Me-4-CF3 OMe 2-Me-4-CF3 Br 2-Me-4-OCF3 I 2-Me-4-OCF3 OMe 2-Me-4-OCF3 Br 2-Me-4-OCF2H I 2-Me-4-OCF2H OMe 2-Me-4-OCF2H Br 2-Me-4-OCH2CF3 I 2-Me-4-OCH2CF3 OMe 2-Me-4-OCH2CF3 Br 2-Me-4-SCF3 I 2-Me-4-SCF3 OMe 2-Me-4-SCF3 Br 2-Me-4-SOCF3 I 2-Me-4-SOCF3 OMe 2-Me-4-SOCF3

Br 2-Me-4-SO2CF3 I 2-Me-4-SO2CF3 OMe 2-Me-4-SO2CF3 Br 2-Me-4-SCF2H I 2-Me-4-SCFoH OMe 2-Me-4-SCF2H Br 2-Me-4-SOCF2H I 2-Me-4-SOCF2H OMe 2-Me-4-SOCF2H Br 2-Me-4-SO2CF2H I 2-Me-4-SO2CF2H OMe 2-Me-4-SO2CFoH CF3 2-Me-4-CF3 NO2 2-Me-4-CF3 SMe 2-Me-4-CF3 CF3 2-Me-4-OCF3 NO 2-Me-4-OCF3 SMe 2-Me-4-OCF3 CF3 2-Me-4-OCF2H N02 2-Me-4-OCF2H SMe 2-Me-4-OCF2H CF3 2-Me-4-OCH2CF3 No2 2-Me-4-OCH2CF3 SMe 2-Me-4-OCH2CF3 CF3 2-Me-4-SCF3 No2 2-Me-4-SCF3 SMe 2-Me-4-SCF3 CF3 2-Me-4-SOCF3 No2 2-Me-4-SOCF3 SMe 2-Me-4-SOCF3 CF3 2-Me-4-SO2CF3 No2 2-Me-4-SO2CF3 SMe 2-Me-4-SO2CF3 CF3 2-Me-4-SCF2H NO 2-Me-4-SCF2H SMe 2-Me-4-SCF2H CF3 2-Me-4-SOCF2H NO2 2-Me-4-SOCF2H SMe 2-Me-4-SOCF2H CF3 2-Me-4-SO2CF2H N02 2-Me-4-S02CF2H SMe 2-Me-4-SO2CF2H Formulation/Utility Compounds of this invention will generally be used as a formulation or composition with an agriculturally suitable carrier comprising at least one of a liquid diluent, a solid diluent or a surfactant. The formulation or composition ingredients are selected to be consistent with the physical properties of the active ingredient, mode of application and environmental factors such as soil type, moisture and temperature. Useful formulations include liquids such as solutions (including emulsifiable concentrates), suspensions, emulsions (including microemulsions and/or suspoemulsions) and the like which optionally can be thickened into gels. Useful formulations further include solids such as dusts, powders, granules, pellets, tablets, films, and the like which can be water-dispersible ("wettable") or water-soluble. Active ingredient can be (micro) encapsulated and further formed into a suspension or solid formulation; alternatively the entire formulation of active ingredient can be encapsulated (or"overcoated"). Encapsulation can control or delay release of the active ingredient. Sprayable formulations can be extended in suitable media and used at spray volumes from about one to several hundred liters per hectare. High-strength compositions are primarily used as intermediates for further formulation.

The formulations will typically contain effective amounts of active ingredient, diluent and surfactant within the following approximate ranges that add up to 100 percent by weight.

Weight Percent Active Ingredient Diluent Surfactant Water-Dispersible and Water-soluble 5-90 0-94 1-15 Granules, Tablets and Powders.

Suspensions, Emulsions, Solutions 5-50 40-95 0-15 (including Emulsifiable Concentrates) Dusts 1-25 70-99 0-5 Granules and Pellets 0.01-99 5-99.99 0-15 High Strength Compositions 90-99 0-10 0-2 Typical solid diluents are described in Watkins, et al., Ha7ldbook of I71secticide Dust Diluents and Carriers, 2nd Ed., Dorland Books, Caldwell, New Jersey. Typical liquid diluents are described in Marsden, Solve7lts Gllide, 2nd Ed., Interscience, New York, 1950.

McCutcheon's Detergents and Emulsifiers Annual, Allured Publ. Corp., Ridgewood, New Jersey, as well as Sisely and Wood, Encyclopeelia of Slwrface Active Agents, Chemical Publ.

Co., Inc., New York, 1964, list surfactants and recommended uses. All formulations can contain minor amounts of additives to reduce foam, caking, corrosion, microbiological growth and the like, or thickeners to increase viscosity.

Surfactants include, for example, polyethoxylated alcohols, polyethoxylated alkylphenols, polyethoxylated sorbitan fatty acid esters, dialkyl sulfosuccinates, alkyl sulfates, alkylbenzene sulfonates, organosilicones, N, N-dialkyltaurates, lignin sulfonates, naphthalene sulfonate formaldehyde condensates, polycarboxylates, and polyoxyethylene/polyoxypropylene block copolymers. Solid diluents include, for example, clays such as bentonite, montmorillonite, attapulgite and kaolin, starch, sugar, silica, talc, diatomaceous earth, urea, calcium carbonate, sodium carbonate and bicarbonate, and sodium sulfate. Liquid diluents include, for example, water, N, N-dimethylformamide, dimethyl sulfoxide, N-alkylpyrrolidone, ethylene glycol, polypropylene glycol, paraffins, alkylbenzenes, alkylnaphthalenes, oils of olive, castor, linseed, tung, sesame, corn, peanut, cotton-seed, soybean, rape-seed and coconut, fatty acid esters, ketones such as cyclohexanone, 2-heptanone, isophorone and 4-hydroxy-4-methyl-2-pentanone, and alcohols such as methanol, cyclohexanol, decanol and tetrahydrofurfuryl alcohol.

Solutions, including emulsifiable concentrates, can be prepared by simply mixing the ingredients. Dusts and powders can be prepared by blending and, usually, grinding as in a hammer mill or fluid-energy mill. Suspensions are usually prepared by wet-milling; see, for example, U. S. 3,060,084. Granules and pellets can be prepared by spraying the active material upon preformed granular carrier or by agglomeration techniques. See Browning, "Agglomeration", Chemical Engineering, December 4,1967, pp 147-48, Perry's Claerraical

Engineer's Handbook, 4th Ed., McGraw-Hill, New York, 1963, pages 8-57 and following, and PCT Publication WO 91/13546. Pellets can be prepared as described in U. S. 4,172,714.

Water-dispersible and water-soluble granules can be prepared as taught in U. S. 4,144,050, U. S. 3,920,442 and DE 3, 246, 493. Tablets can be prepared as taught in U. S. 5,180,587, U. S.

5,232,701 and U. S. 5,208,030. Films can be prepared as taught in GB 2,095,558 and U. S.

3,299,566.

For further information regarding the art of formulation, see T. S. Woods,"The Formulator's Toolbox-Product Forms for Modern Agriculture"in Pesticide Chemistry and Bioscience, The Food-Environment Challenge, T. Brooks and T. R. Roberts, Eds., Proceedings of the 9th International Congress on Pesticide Chemistry, The Royal Society of Chemistry, Cambridge, 1999, pp. 120-133. See also U. S. 3,235,361, Col. 6, line 16 through Col. 7, line 19 and Examples 10-41 ; U. S. 3,309,192, Col. 5, line 43 through Col. 7, line 62 and Examples 8, 12,15,39,41,52,53,58,132,138-140,162-164,166,167 and 169-182 ; U. S. 2,891,855, Col. 3, line 66 through Col. 5, line 17 and Examples 1-4 ; Klingman, steed Control as a Science, John Wiley and Sons, Inc., New York, 1961, pp 81-96; and Hance et al., Weed Cotiti-ol Haiidbook, 8th Ed., Blackwell Scientific Publications, Oxford, 1989. hi the following Examples, all percentages are by weight and all formulations are prepared in conventional ways. Compound numbers refer to compounds in Index Tables A-D.

Example A Wettable Powder Compound 7 65.0% dodecylphenol polyethylene glycol ether 2.0% sodium ligninsulfonate 4.0% sodium silicoaluminate 6.0% montmorillonite (calcined) 23.0%.

Example B Granule Compound 7 10.0% attapulgite granules (low volatile matter, 0.71/0.30 mm ; U. S. S. No. 25-50 sieves) 90.0%.

Example C Extruded Pellet Compound 7 25.0% anhydrous sodium sulfate 10.0% crude calcium ligninsulfonate 5.0% sodium alkylnaphthalenesulfonate 1.0% calcium/magnesium bentonite 59.0%.

Example D Emulsifiable Concentrate Compound 7 20. 0% blend of oil soluble sulfonates and polyoxyethylene ethers 10.0% isophorone 70.0%.

Example E Granule Compound 7 0.5% cellulose 2.5% lactose 4. 0% cornmeal 93.0%.

Compounds of this invention are characterized by favorable metabolic and/or soil residual patterns and exhibit activity controlling a spectrum of agronomic and non- agronomic invertebrate pests. (In the context of this disclosure"invertebrate pest control" means inhibition of invertebrate pest development (including mortality) that causes significant reduction in feeding or other injury or damage caused by the pest; related expressions are defined analogously.) As referred to in this disclosure, the term "invertebrate pest"includes arthropods, gastropods and nematodes of economic importance as pests. The term"arthropod"includes insects, mites, spiders, scorpions, centipedes, millipedes, pill bugs and symphylans. The term"gastropod"includes snails, slugs and other Stylommatophora. The tenn"nematode"includes all of the helminths, such as: roundworms, heartworms, and phytophagous nematodes (Nematoda), flukes (Tematoda), Acanthocephala, and tapeworms (Cestoda). Those skilled in the art will recognize that not all compounds are equally effective against all pests. Compounds of this invention display activity against economically important agronomic, forest, greenhouse, nursery, ornamentals, food and fiber, public and animal health, domestic and commercial structure, household, and stored product pests. These include larvae of the order Lepidoptera, such as armyworms, cutworms, loopers, and heliothines in the family Noctuidae (e. g., fall armyvvorm (Sporloptet°a fitgipenda J. E. Smith), beet armyworm (Spodoptera exigua

Hiibner), black cutworm (Agrotis ipsilori Hufnagel), cabbage looper (Trchoplusia ni Huber), tobacco budworm (Heliothis virescens Fabricius)); borers, casebearers, webworms, coneworms, cabbageworms and skeletonizers from the family Pyralidae (e. g., European corn borer (Ostrinia nubilalis Hübner), navel orangewonn (Amyelois transitella Walker), corn root webworm (Crambus caligiftosellus Clemens), sod webworm (Herpetogramma licarsisalis Walker)); leafrollers, budwonns, seed worms, and fruit worms in the family Tortricidae (e. g., codling moth (Cvdiapomojaella Limmaeus), grape berry moth (Endopiza viteana Clemens), oriental fruit moth (Grapholita molesta Busck) ; and many other economically important lepidoptera (e. g., diamondback moth (Plutella xylostella Linnaeus), pink bollworm (Pectnophora gossypiella Saunders), gypsy moth (Lymantria dispar Linnaeus)); nymphs and adults of the order Blattodea including cockroaches from the families Blattellidae and Blattidae (e. g., oriental cockroach (Blatta orientalis Linnaeus), Asian cockroach (Blatella asahinai Mizukubo), German cockroach (Blattella germanica Linnaeus), brownbanded cockroach (Siipella loizgipalpa Fabricius), American cockroach (Periplaneta americana Linnaeus), brown cockroach (Periplaneta brunnea Burmeister), Madeira cockroach (Leucophaea maderae Fabricius)); foliar feeding larvae and adults of the order Coleoptera including weevils from the families Anthribidae, Bruchidae, and Curculionidae (e. g., boll weevil (Anthonomus grandis Boheman), rice water weevil (Lissorhoptrus oryzophilus Kuschel), granary weevil (Sitophilus granarius Linnaeus), rice weevil (Sitophilus olyzae Linnaeus)); flea beetles, cucumber beetles, rootworms, leaf beetles, potato beetles, and leafminers in the family Chrysomelidae (e. g., Colorado potato beetle (Leptinotarsa decemilineata Say), western corn rootworm (Diabrotica virgifera virgifera LeConte)); chafers and other beetles from the family Scaribaeidae (e. g., Japanese beetle (Popillia jccponica Newman) and European chafer (Rhizotrogus majalis Razoumowsky)); carpet beetles from the family Dermestidae; wireworms from the family Elateridae; bark beetles from the family Scolytidae and flour beetles from the family Tenebrionidae. In addition it includes: adults and larvae of the order Dermaptera including earwigs from the family Forficulidae (e. g., European earwig (Forficula auricularia Linnaeus), black earwig (Clzelisoches morio Fabricius)) ; adults and nymphs of the orders Hemiptera and Homoptera such as, plant bugs from the family Miridae, cicadas from the family Cicadidae, leaflioppers (e. g. E7npoasca spp.) from the family Cicadellidae, planthoppers from the families Fulgoroidae and Delphacidae, treehoppers from the family Membracidae, psyllids from the family Psyllidae, whiteflies from the family Aleyrodidae, aphids from the family Aphididae, phylloxera from the family Phylloxeridae, mealybugs from the family Pseudococcidae, scales from the families Coccidae, Diaspididae and Margarodidae, lace bugs from the family Tingidae, stink bugs from the family Pentatomidae, cinch bugs (e. g., Blissus spp.) and other seed bugs from the family Lygaeidae, spittlebugs from the family Cercopidae squash bugs from the family Coreidae, and red bugs and cotton

stainers from the family Pyrrhocolidae. Also included are adults and larvae of the order Acari (mites) such as spider mites and red mites in the family Tetranychidae (e. g., European red mite (Panonychus ulmi Koch), two spotted spider mite (Tetranychus urticae Koch), McDaniel mite (Tetranychus mcdanieli McGregor)), flat mites in the family Tenuipalpidae (e. g., citrus flat mite (Brevipalpus lewisi McGregor)), rust and bud mites in the family Eriophyidae and other foliar feeding mites and mites important in human and animal health, i. e. dust mites in the family Epidermoptidae, follicle mites in the family Demodicidae, grain mites in the family Glycyphagidae, ticks in the order Ixodidae (e. g., deer tick (Ixodes scapulairs Say), Australian paralysis tick (Ixodes holocyclus Neumann), American dog tick (Dermacentor variabilis Say), lone star tick (Amblyomma americanum Linnaeus) and scab and itch mites in the families Psoroptidae, Pyemotidae, and Sarcoptidae; adults and immatures of the order Orthoptera including grasshoppers, locusts and crickets (e. g., migratory grasshoppers (e. g., Melanoplus sanguinipes Fabricius, M. differentialis Thomas), American grasshoppers (e. g., Schistocerca americana Drury), desert locust (Schistocerca gregaria Forskal), migratory locust (Locusta migratoria Linnaeus), house cricket (Acheta domesticus Linnaeus), mole crickets (Gryllotalpa spp.)); adults and immatures of the order Diptera including leafininers, midges, fruit flies (Tephritidae), frit flies (e.g., Oscinella frit Linnaeus), soil maggots, house flies (e. g., A4'tisca do7iiestica Linnaeus), lesser house flies (e. g., Fannia caniculairs Linnaeus, F. femoralis Stein), stable flies (e.g., Stomoxys calcitrans Linnaeus), face flies, horn flies, blow flies (e. g., Chrysomya spp., Phormia spp.), and other muscoid fly pests, horse flies (e. g., Tabanzus spp.), bot flies (e. g., Gastrophilus spp., Oestrus spp.), cattle grubs (e. g., Hypoderma spp.), deer flies (e. g., Chrysops spp.), keds (e. g., Melophagus ovinus Linnaeus) and other Brachycera, mosquitoes (e. g., Aedes spp., Anopheles spp., Culex spp.), black flies (e. g., Prosimulium spp., Simulium spp.), biting midges, sand flies, sciarids, and other Nematocera; adults and immatures of the order Thysanoptera including onion thrips (Thrips tabaci Lindeman) and other foliar feeding thrips; insect pests of the order Hymenoptera including ants (e. g., red carpenter ant (Camponotus ferrugineus Fabricius), black carpenter ant (Camponotus pennsylvanictss De Geer), Pharaoh ant (Monomorium pharaonis Linnaeus), little fire ant (Wasiliallilia auropunctata Roger), fire ant (Solenopsis geminata Fabricius), red imported fire ant (Solenopsis iizvicta Buren), Argentine ant (Iridomyrmex humilis Mayr), crazy ant (Paratrechina longicornis Latreille), pavement ant (Tetramorium caespitum Linnaeus), cornfield ant (Lasius alienus Förster), odorous house ant (Tapinoma sessile Say)), bees (including carpenter bees), hornets, yellow jackets and wasps; insect pests of the order Isoptera including the eastern subterranean termite (Reticulitermes flavipes Kollar), western subterranean termite (Reticulitermes hesperus Banks), Formosan subterranean termite (Coptotermes formosanus Shiraki), West Indian drywood tennite (Incisitermes immigrans Snyder) and other termites of economic importance; insect pests of the order Thysanura such

as silverfish (Lepisma saccharina Linnaeus) and firebrat (Thermobia domestica Packard) ; insect pests of the order Mallophaga and including the head louse (Pediculus humans capitis De Geer), body louse (Pediculus humans humans Linnaeus), chicken body louse (Menacanthus stramineus Nitszch), dog biting louse (Ti-ichodectes caiiis De Geer), fluff louse (Goniocotes gallinae De Geer), sheep body louse (Bovicola ovis Schrank), short-nosed cattle louse (Haematopinus eurysternus Nitzsch), long-nosed cattle louse (Linognathus vituli Linnaeus and other sucking and chewing parasitic lice that attack man and animals; insect pests of the order Siphonoptera including the oriental rat flea (Xenopsylla cheopis Rothschild), cat flea (Ctenocephalides felis Bouche), dog flea (Ctenocephalides canis Curtis), hen flea (Ceratophyllus gallinae Schrank), sticktight flea (Echidlnophaga gallinacea Westwood), human flea (Pulex irritans Linnaeus) and other fleas afflicting mammals and birds. Additional arthropod pests covered include: spiders in the order Araneae such as the brown recluse spider (Loxosceles reclusa Gertsch & Mulaik) and the black widow spider (Latrodectus mactans Fabricius), and centipedes in the order Scutigeromorpha such as the house centipede (Scutigera coleoptrata Linnaeus). Activity also includes members of the Classes Nematoda, Cestoda, Trematoda, and Acanthocephala including economically important members of the orders Strongylida, Ascaridida, Oxyurida, Rhabditida, Spirurida, and Enoplida such as but not limited to economically important agricultural pests (i. e. root knot nematodes in the genus Ateloidogy7le, lesion nematodes in the genus Pratylenchus, stubby root nematodes in the genus Trichodorus, etc.) and animal and human health pests (i. e. all economically important flukes, tapeworms, and roundworms, such as Stronglylus vulgaris in horses, Toxocara canis in dogs, Haemonchus Contortus in sheep, Dirofilaria i7niitis Leidy in dogs, Anoplocephala perfoliata in horses, Fasciola hepatica Linnaeus in ruminants, etc.).

Compounds of the invention show particularly high activity against pests in the order Lepidoptera (e. g., Alaba7na argillacea Hübner (cotton leaf worm), Archips argyrospila Walker (fruit tree leaf roller), A. rosana Linnaeus (European leaf roller) and other Al-chips species, Chilo suppressalis Walker (rice stem borer), Cnaphalocrosis medinalis Guenee (rice leaf roller), Crambus caliginosellus Clemens (corn root webworm), Crambus tetrrelus Zincken (bluegrass webworm), Cvdia pomonella Linnaeus (codling moth), Earias insulana Boisduval (spiny bollworm), Earias vittella Fabricius (spotted bollworm), Helicove7pa armigera Hübner (American bollworm), Helicoveya zea Boddie (corn earworm), Heliothis virescens Fabricius (tobacco budworm), Herpetogramma licarsisalis Walker (sod webworm), Lobesia boti-aiia Denis & Schiffermuller (grape berry moth), Pectinophora gossvpiella Saunders (pink bollworm), Phyllocnistis citrella Stainton (citrus leafininer), Pieris brassicae Linnaeus (large white butterfly), Pieris rapae Linnaeus (small white butterfly), Pllltella aylostella Linnaeus (diamondback moth), Spodoptera exigua Hübber (beet armyworm), Spodoptera litura Fabricius (tobacco cutworm, cluster caterpillar),

Spodoptera frugiperda J. E. Smith (fall armyworm), Trichoplusia ni Hübner (cabbage looper) and Tuta absoluta Meyrick (tomato leafminer)). Compounds of the invention also have commercially significant activity on members from the order Homoptera including: Acyrthisiphon pisum Harris (pea aphid), Aphis craccivora Koch (cowpea aphid), Aphis fabae Scopoli (black bean aphid), Aphis-ossi'ii Glover (cotton aphid, melon aphid), Aphis pomi De Geer (apple aphid), Aphis spiraecola Patch (spirea aphid), Aulacorthum solani Kaltenbach (foxglove aphid), Chaetosiphon fragaefolii Cockerell (strawberry aphid), Diuraphis noxia Kurdjumov/Mordvilko (Russian wheat aphid), Dysaphis plantaginea Paaserini (rosy apple aphid), Eriosoma lanigerum Hausmann (woolly apple aphid), Hyalopterus pruni Geoffroy (mealy plum aphid), Lipaphis erysimi Kaltenbach (turnip aphid), Metopolophium dirrhodum Walker (cereal aphid), Macrosipum euphorbiae Thomas (potato aphid), Myzus persicae Sulzer (peach-potato aphid, green peach aphid), Nasonovia ribisnigri Mosley (lettuce aphid), Penzplaigacs spp. (root aphids and gall aphids), Rhopalosiphum maidis Fitch (corn leaf aphid), Rhopalosipliuni padi Linnaeus (bird cherry- oat aphid), Schizaphis graminum Rondani (greenbug), Sitobioii aveiiae Fabricius (English grain aphid), Therioaphis maculata Buckton (spotted alfalfa aphid), Toxoptera aurantii Boyer de Fonscolombe (black citrus aphid), and Toxoptera citricida Kirkaldy (brown citrus aphid); Adelges spp. (adelgids); Phylloxera devastatrix Pergande (pecan phylloxera) ; Bemisia tabaci Gennadius (tobacco whitefly, sweetpotato whitefly), Bemisia argentifolii Bellows & Perring (silverleaf whitefly), Dialeurodes citri Ashmead (citrus whitefly) and Trialeurodes vaporariorum Westwood (greenhouse whitefly) ; Empoasca fabae Harris (potato leafhopper), Laodelphax stf-iatellzis Fallen (smaller brown planthopper), Macrolestes quadrilineatus Forbes (aster leafhopper), Nephotettix cititiceps LThler (green leafliopper), Nephotettix nigropictus Stål (rice leafhopper), Nilaparvata lugens Stål (brown planthopper), Peregrinus maidis Ashmead (corn planthopper), Sogatella furcifera Horvath (white-backed planthopper), Sogatodes orizicola Muir (rice delphacid), Typhlocyba pomaria McAtee white apple leafhopper, Erythroneoura spp. (grape leafhoppers); Alfagicidada septeitdeciiii Linnaeus (periodical cicada); Icerya pzii-chasi Maskell (cottony cushion scale), Quadraspidiotus perniciosus Comstock (San Jose scale); Planococcrrs citri Risso (citrus mealybug); Pseudococcus spp. (other mealybug complex) ; Cacopsylla pyricola Foerster (pear psylla), Trioza diospyri Ashmead (persimmon psylla). These compounds also have activity on members from the order Hemiptera including: Acrosternum hilare Say (green stink bug), Arasa tristis De Geer (squash bug), Blissus leucopterus leucopterus Say (chinch bug), Corythuca gossypii Fabricius (cotton lace bug), Cyrtopeltis modesta Distant (tomato bug), Dysdercus suturellus Herrich-Schäffer (cotton stainer), Euchistus servus Say (brown stink bug), Euchistus variolarius Palisot de Beauvois (one-spotted stink bug), Graptosthetzrs spp. (complex of seed bugs), Leptoglossus corculus Say (leaf-footed pine seed bug), Lygus lineolaf-is Palisot de Beauvois (tarnished plant bug), Nezara viridula Linnaeus (southern

green stink bug), Oebalzcs pugnczx Fabricius (rice stink bug), Oticopeltzisfasciatus Dallas (large milkweed bug), Pseacdatonioscelis seriatzrs Reuter (cotton fleahopper). Other insect orders controlled by compounds of the invention include Thysanoptera (e. g., Frankliniella occide71talis Pergande (western flower thrip), Scirthothrips citri Moulton (citrus thrip), Sericothrips variabilis Beach (soybean thrip), and Thrips tabaci Lindeman (onion thrip); and the order Coleoptera (e. g., Leptinotarsa decemlineata Say (Colorado potato beetle), Epilachua varivestis Mulsant (Mexican bean beetle) and wireworms of the genera Agriotes, Athous or Limo7lilJs).

Compounds of Formula I can also be mixed with one or more other biologically active compounds or agents including insecticides, fungicides, nematocides, bactericides, acaricides, growth regulators such as rooting stimulants, chemosterilants, semiochemicals, repellents, attractants, pheromones, feeding stimulants, other biologically active compounds or entomopathogenic bacteria, virus or fungi to form a multi-component pesticide giving an even broader spectrum of agricultural utility. Thus the present invention also relates to a method wherein the invertebrate pest or its environment is contacted with a biologically effective amount of a compound of Formula I or a composition comprising a compound of Formula I and a biologically effective amount of at least one additional compound or agent for controlling invertebrate pests. Likewise compositions of the present invention comprising a compound of Formula la can further comprise a biologically effective amount of at least one additional biologically active compound or agent. Examples of such biologically active compounds or agents with which compounds of this invention can be formulated are: insecticides such as abamectin, acephate, acetamiprid, avermectin, azadirachtin, azinphos-methyl, bifenthrin, binfenazate, buprofezin, carbofuran, chlorfenapyr, chlorfluazuron, chlorpyrifos, chlorpyrifos-methyl, chromafenozide, clothianidin, cyfluthrin, beta-cyfluthrin, cyhalothrin, lambda-cyhalothrin, cypermethrin, cyromazine, deltamethrin, diafenthiuron, diazinon, diflubenzuron, dimethoate, diofenolan, emamectin, endosulfan, esfenvalerate, ethiprole, fenothicarb, fenoxycarb, fenpropathrin, fenproximate, fenvalerate, fipronil, flonicamid, flucythrinate, tau-fluvalinate, flufenoxuron, fonophos, halofenozide, hexaflumuron, imidacloprid, indoxacarb, isofenphos, lufenuron, malathion, metaldehyde, methamidophos, methidathion, methyl, methoprene, methoxychlor, monocrotophos, methoxyfenozide, nithiazin, novaluron, oxamyl, parathion, parathion-methyl, permethrin, phorate, phosalone, phosmet, phosphamidon, pirimicarb, profenofos, pymetrozine, pyridalyl, pyriproxyfen, rotenone, spinosad, sulprofos, tebufenozide, teflubenzuron, tefluthrin, terbufos, tetrachlorvinphos, thiacloprid, thiamethoxam, thiodicarb, thiosultap-sodium, tralomethrin, trichlorfon and triflumuron; fungicides such as acibenzolar, azoxystrobin, benomyl, blasticidin-S, Bordeaux mixture (tribasic copper sulfate), bromuconazole, carpropamid, captafol, captan, carbendazim, chloroneb, chlorothalonil, copper oxychloride, copper salts, cyflufenamid, cymoxanil, cyproconazole, cyprodinil, (S)-3, 5-dichloro-N-(3-

chloro-1-ethyl-1-methyl-2-oxopropyl)-4-methylbenzamide (RH 7281), diclocymet (S-2900), diclomezine, dicloran, difenoconazole, (S)-3, 5-dihydro-5-methyl-2- (methylthio)-5-phenyl-3- (phenylamino)-4H-imidazol-4-one (RP 407213), dimethomorph, dimoxystrobin, diniconazole, diniconazole-M, dodine, edifenphos, epoxiconazole, famoxadone, fenamidone, fenarimol, fenbuconazole, fencaramid (SZX0722), fenpiclonil, fenpropidin, fenpropimorph, fentin acetate, fentin hydroxide, fluazinam, fludioxonil, flumetover (RPA 403397), fluquinconazole, flusilazole, flutolanil, flutriafol, folpet, fosetyl-aluminum, furalaxyl, furametapyr (S-82658), hexaconazole, ipconazole, iprobenfos, iprodione, isoprothiolane, kasugamycin, kresoxim-methyl, mancozeb, maneb, mefenoxam, mepronil, metalaxyl, metconazole, metominostrobin/fenominostrobin (SSF-126), myclobutanil, neo-asozin (ferric methanearsonate), oxadixyl, penconazole, pencycuron, probenazole, prochloraz, propamocarb, propiconazole, pyrifenox, pyraclostrobin, pyrimethanil, pyroquilon, quinoxyfen, spiroxamine, sulfur, tebuconazole, tetraconazole, thiabendazole, thifluzamide, thiophanate-methyl, thiram, tiadinil, triadimefon, triadimenol, tricyclazole, trifloxystrobin, triticonazole, validamycin and vinclozolin ; nematocides such as aldicarb, oxamyl and fenamiphos ; bactericides such as streptomycin; acaricides such as amitraz, chinomethionat, chlorobenzilate, cyhexatin, dicofol, dienochlor, etoxazole, fenazaquin, fenbutatin oxide, fenpropathrin, fenpyroximate, hexythiazox, propargite, pyridaben and tebufenpyrad; and biological agents such as Bacilltrs thui-ii7gietisis including ssp. aizawai and kaifstaki, Bacillzts thuringiensis delta endotoxin, baculovirus, and entomopathogenic bacteria, virus and fungi.

A general reference for these agricultural protectants is Tlze Pesticide Matual, l2th Editioiz, C. D. S. Tomlin, Ed., British Crop Protection Council, Farnham, Surrey, U. K., 2000.

Preferred insecticides and acaricides for mixing with compounds of Fonnula I or la include pyrethroids such as cypermethrin, cyhalothrin, cyfluthrin, beta-cyfluthrin, esfenvalerate, fenvalerate and tralomethrin; carbamates such as fenothicarb, methyl, oxamyl and thiodicarb ; neonicotinoids such as clothianidin, imidacloprid and thiacloprid ; neuronal sodium channel blockers such as indoxacarb; insecticidal macrocyclic lactones such as spinosad, abamectin, avermectin and emamectin ; y-aminobutyric acid (GABA) antagonists such as endosulfan, ethiprole and fipronil; insecticidal ureas such as flufenoxuron and triflumuron ; juvenile hormone mimics such as diofenolan and pyriproxyfen; pymetrozine ; and amitraz. Preferred biological agents for mixing with compounds of Formula I or la include Bacillus thuringiensis and Bacillus thuringiensis delta endotoxin as well as naturally occurring and genetically modified viral insecticides including members of the family Baculoviridae as well as entomophagous fungi.

Most preferred mixtures include a mixture of a compound of Formula I or la with cyhalothrin ; a mixture of a compound of Formula I or Ia with beta-cyfluthrin ; a mixture of a compound of Formula I or la with esfenvalerate; a mixture of a compound of Formula I or la

with methomyl ; a mixture of a compound of Formula I or la with imidacloprid; a mixture of a compound of Formula I or la with thiacloprid; a mixture of a compound of Formula I or Ia with indoxacarb; a mixture of a compound of Formula I or la with abamectin ; a mixture of a compound of Formula I or Ia with endosulfan; a mixture of a compound of Formula I or Ia with ethiprole; a mixture of a compound of Formula I or la with fipronil; a mixture of a compound of Formula I or la with flufenoxuron ; a mixture of a compound of Formula I or la with pyriproxyfen ; a mixture of a compound of Formula I or la with pymetrozine; a mixture of a compound of Formula I or la with amitraz; a mixture of a compound of Formula I or Ia with Bacillus thziritigieiisis and a mixture of a compound of Formula I or la with Bacillus thztsrifigiensis delta endotoxin.

In certain instances, combinations with other invertebrate pest control compounds or agents having a similar spectrum of control but a different mode of action will be particularly advantageous for resistance management. Thus, compositions of the present invention comprising a compound of Formula la can further comprise a biologically effective amount of at least one additional invertebrate pest control compound or agent having a similar spectrum of control but a different mode of action, and the methods of the present invention can utilize compositions compromising a compound of Formula I and a biologically effective amount of at least one additional invertebrate pest control compound or agent having a similar spectrum of control but a different mode of action. Contacting a plant genetically modified to express a plant protection compound (e. g., protein) or the locus of the plant with a biologically effective amount of a compound of Formula I or la can also provide a broader spectrum of plant protection and be advantageous for resistance management.

Invertebrate pests are controlled and protection of agronomic, horticultural and specialty crops, animal and human health is achieved by applying one or more of the compounds of Formula I or Ia, in an effective amount, to the environment of the pests including the agronomic and/or nonagronomic locus of infestation, to the area to be protected, or directly on the pests to be controlled. Thus, the present invention comprises a method for the control of foliar-and soil-inhabiting invertebrates and protection of agronomic and/or nonagronomic crops, comprising contacting the invertebrates or their environment with a biologically effective amount of one or more of the compounds of Formula I, or with a composition comprising at least one such compound or a composition comprising at least one such compound and an effective amount of at least one additional biologically active compound or agent. A preferred method of contact is by spraying.

Alternatively, a granular composition comprising a compound of Formula I or la can be applied to the plant foliage or the soil. Compounds of Formula I or Ia are effective in delivery through plant uptake by contacting the plant with a composition comprising a compound of Formula I or la applied as a soil drench of a liquid formulation, a granular

formulation to the soil, a nursery box treatment or a dip of transplants. Other methods of contact include application of a compound of Formula I or Ia or a composition comprising of Formula I or Ia of the invention by direct and residual sprays, aerial sprays, seed coats, microencapsulations, systemic uptake, baits, eartags, boluses, foggers, fumigants, aerosols, dusts and many others.

The compounds of Formula I or la can be incorporated into baits that are consumed by the invertebrates or within devices such as traps and the like. Granules or baits comprising between 0.01-5% active ingredient, 0.05-10% moisture retaining agent (s) and 40-99% vegetable flour are effective in controlling soil insects at very low application rates, particularly at doses of active ingredient that are lethal by ingestion rather than by direct contact.

The compounds of Formula I or la can be applied in their pure state, but most often application will be of a formulation comprising one or more compounds with suitable carriers, diluents, and surfactants and possibly in combination with a food depending on the contemplated end use. A preferred method of application involves spraying a water dispersion or refined oil solution of the compounds. Combinations with spray oils, spray oil concentrations, spreader stickers, adjuvants, other solvents, and synergists such as piperonyl butoxide often enhance compound efficacy.

The rate of application required for effective control (i. e."biologically effective amount") will depend on such factors as the species of invertebrate to be controlled, the pest's life cycle, life stage, its size, location, time of year, host crop or animal, feeding behavior, mating behavior, ambient moisture, temperature, and the like. Under normal circumstances, application rates of about 0.01 to 2 kg of active ingredient per hectare are sufficient to control pests in agronomic ecosystems, but as little as 0.0001 kg/hectare may be sufficient or as much as 8 kg/hectare may be required. For nonagronomic applications, effective use rates will range from about 1.0 to 50 mg/square meter but as little as 0.1 mg/square meter may be sufficient or as much as 150 mg/square meter may be required.

One skilled in the art can easily determine the biologically effective amount necessary for the desired level of invertebrate pest control.

The following Tests in the Biological Examples of the Invention demonstrate the efficacy of methods of the invention for protecting plants from specific arthropod pests.

"Control efficacy"represents inhibition of arthropod development (including mortality) that causes significantly reduced feeding. The pest control protection afforded by the compounds is not limited, however, to these species. See Index Tables A-D for compound descriptions.

The following abbreviations are used in the Index Tables which follows: t is tertiary, iz is normal, i is iso, s is secondary, c is cyclo, Me is methyl, Et is ethyl, Pr is propyl and Bu is butyl; accordingly i-Pr is isopropyl, s-Bu is secondary butyl, etc. The abbreviation "Ex."stands for"Example"and is followed by a number indicating in which example the compound is prepared.

Index Table A Compound R3 R4 R5a R5b mp °C 1 i-Pr 2-Me H 4-OCF3 oil 2 i-Pr 2-Me H 4-CF3 oil 3 (Ex. 1) i-Pr 2-Me 2-Me 4-CF3 100-103 Index Table B Compound R3 R4 Q X Y Z mp °C 4 i-Pr Cl NPh N CH CCF3 155-159 Index Table C Compound R3 R4 W X Y Z R5 m.p. °C 5 i-Pr Me C-Me N CH CH CF3 132-135 6 i-Pr Me C-Et N CH CH Cl 127-131 Index Table D Compound R3 R4a R4b R6 R7 V mp °C 7 (Ex. 3) Me Cl H Cl CF3 N 155-159 8 i-Pr Me H H CF3 CH 9 CH2CHClCH3 Me H Cl CF3 CH 178-180 10 (Ex. 2) Me Me ci Cl CF3 N solid 11 i-Pr Me Cl Cl Br N 190-193 Index Table E

Compound R3 R4a R6 R7 V mp °C 12 CHoC-CH Me Cl Br CH 13 CH2C_CH Me Cl CF3 CH BIOLOGICAL EXAMPLES OF THE INVENTION TEST For evaluating control of diamondback moth (Plzstella. ylo, rtella) the test unit consisted of a small open container with a 12-14-day-old radish plant inside. This was pre-infested with 10-15 neonate larvae on a piece of insect diet by use of a core sampler to remove a plug from a sheet of hardened insect diet having many larvae growing on it and transfer the plug containing larvae and diet to the test unit. The larvae moved onto the test plant as the diet plug dried out.

Test compounds were formulated using a solution containing 10% acetone, 90% water and 300 ppm X-77@ Spreader Lo-Foam Formula non-ionic surfactant containing alkylarylpolyoxyethylene, free fatty acids, glycols and isopropanol (Loveland Industries, Inc.), unless otherwise indicated. The formulated compounds were applied in 1 mL of liquid through a SUJ2 atomizer nozzle with 1/8 JJ custom body (Spraying Systems Co.) positioned 1.27 cm (0.5 inches) above the top of each test unit. All experimental compounds in this screen were sprayed at 250 ppm and replicated three times. After spraying of the formulated test compound, each test unit was allowed to dry for 1 hour and then a black, screened cap was placed on top. The test units were held for 6 days in a growth chamber at 25 °C and 70% relative humidity. Plant feeding damage was then visually assessed.

Of the compounds tested, the following provided very good levels of plant protection (20% or less feeding damage) : 3,4,5,6,8 and 10.