PURPOSE: To obtain the subject compd. as an HMG-CaA reductase inhibitor by using a novel intermediate ketone as a starting material, reducing this material and subjecting the reduced ketone to hydrolysis, ring formation, etc.
CONSTITUTION: The obtain objective compd. of formula II [X is CH2-CH2 or CH=CH; A is formula III, formula IV (R7 is H, alkyl; R3 is H)] is obtd. by reducing the ketone of formula I (R1 is cycloalkyl, (substd.) alkyl; R2 is (substd.) heteroaryl or (substd.) aryl; R3, R4 are H, acyl, alkylsulfonyl, aminocarbonyl (substd.) alkyl, etc.; R8↑' is alkyl), hydrolyzing the reduced ketone at need and subjecting the carboxylic acid to ring formation or subjecting -CH=CH- to hydrogenation. The compd. of the formula I is obtd. by bringing the aldehyde of formula VI, obtd. by bringing the pyrrol of formula V into reaction with N,N-dialkylaminoacrolein in the presence of an acid chloride, into reaction with the acetoacetate of formula VII in an inert solvent in the presence of a base.
RORUFU ANGAABAUAA
PEETAA FUAI
HIRUMARU BISHIYOTSUFU
DEIITAA PETSUTSUINA
DERUFU SHIYUMITSUTO
