摘要 |
Title compds. I (R,R1,R2 = H, halogen, methoxy, nitro, C1-6 alkyl; if R2 = H, R and R1 = methylenedioxy, useful as a regulating agent of the stomach and intestines, were prepd. by the reaction of N-(piperid-4-yl)-2-methoxy-4-amino-5-chlorobenzamide(II) and benzylmethane sulfonate(III) in aq. solvent at 50↿-100≰C in the presence of acid-binding agent. Thus a mixt. of 2-methoxy-4-amino-5-chlorobenzoic acid, triethylamine, ethylchloroformate, and 1-ethoxycarbonyl-4-aminopiperidine was reacted to give N-(1-ethoxycarbonyl piperid-4-yl)-2-methoxy-4-amino-5-chlorobenzamide (m.p. 140-142≰C). |