NOVEL PROCESS FOR PRODUCING 2-HYDROXYALKYL-1,4- DIHYDROPYRIDINE-3,5-DICARBOXYLIC ACID DIESTER DERIVATIVE

摘要

PURPOSE:To obtain the titled compound useful as a drug having vasodilating activity, etc. and expected to be useful for the remedy of circulatory diseases, by using a novel enamine compound and a specific acetylene compound as the raw materials, and reacting the materials with a benzylidene compound, etc. CONSTITUTION:The objective compound of formula VI can be produced either by reacting the novel enamine compound of formula I (R4 is lower alkyl, lower haloalkyl, lower alkenyl, lowr alkynyl, aralkyl, aryl, etc.; A is alkylene) with the benzylidene compound of formula II (R1 and R2 are H, Cl, NO2 or CN; when one of R1 and R2 is H, the other is Cl, NO2 or CN, and when one of them is NO2 or CN, the other is H; R3 is same as R4) or with the aldehyde of formula III and beta-ketoester compound of formula IV, or by reacting the acethylene compound of formula V with the benzylidene compound of formula II and NH3 and its salt or the aldehyde compound of formula III, the beta-ketoester compound of formula IV and NH3 and its salt.