PURPOSE: To produce in high yield the compd. having an excellent anti- inflammatory activity, etc., by allowing a substd. indole-3acetic acid being a starting material to react with lithium, then alkylating, esterifying, reducing, condensing with ester and hydrolyzing last of all.
CONSTITUTION: For example, a compd. expressed by formula III is formed by allowing the substd. indole-3-acetic acid expressed by formula II (R4 and R5 are each H, 1-6C lower alkyl or halogen) to react with the lithium, and then the compd. expressed by formula V is obtained by alkylating the compd. expressed by formula III with the compd. expressed by formula IV (R2 is H, 4-halogen, 2- and 4-dihalogen, 3-CF3, 4-OCH3; X is halogen of Cl, Br or I). Then the compd. expressed by formula V is esterified to form the ester expressed by formula VI, then the ester is reduced, then isomers A and B of the compd. expressed by formula IX are obtained by condensing the obtained compd. expressed by formula VII with the compd. expressed by formula VIII (R1 is 1-4C, lower alkyl; R3 is 1-8C lower alkyl). Then the isomer A is crystallized and separated and hydrolyzed to obtain the objective compd. expressed by formula I.
KARERU PERUTSU
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