3-Phenoxymethyl-piperidino 1-heterocyclyl-oxo-propane derivs. - useful as vasodilators and beta adrenergic receptor inhibitors

摘要

Aminopropanol derivs. of formula (I) and their physiologically acceptable salts are new. In (I), R1 and R2 are H, lower alkyl (opt. substd. by OH or alkanoyloxy), or COZ; X is OH, alkoxy or NR6R7; R6 and R7 are H or lower alkyl or hydroxyalkyl; R3 is H or OR8; R8 is H, lower alkanoyl or aroyl opt. substd. by halo lower alkyl or alkoxy, alkoxycarbonyl, OH, alkylthio, CN, NO2 or CF3; R4 and R5 are H, halo, OH, lower alkyl, alkoxy or alkylthio, COOH, benzyloxy, benzyloxycarbonyl or alkoxycarbonyl; X and Y are N or -C(R9)=; R9 is H, lower alkyl opt. substd. by OR8, or COZ. (I) are vasodilators (hypotensives) and inhibitors of beta-adrenergic receptors. In an example, 4- 2-hydroxy-3-(4-phenoxymethylpiperidino)propoxy indole was prepd. from 4-(2,3-epoxypropoxy)indole and 4-phenoxymethyl-piperidine.