Title:
NNACYLLAMINO ACID DERIVATIVE
Document Type and Number:
Japanese Patent JPS5659742
Kind Code:
A
Abstract:
Novel N-acyl amino acid derivatives are irreversible inhibitors of angiotensin-converting enzyme and have the following general Formula 1:- wherein:- Z represents an electron-withdrawing group, preferably cyano or a carbonyl-terminated functional group; X represents a group which, in combination with Z, can form a Michael acceptor after abstraction of the proton from the carbon atom adjacent to X, and preferably X is ethynyl or a fluoromethyl group; R1 represents hydrogen, alkyl or phenylalkyl; and R2 represents an aminocarboxylic acid residue obtained by removal of a hydrogen atom from the amino group thereof. Novel intermediates include compounds of the following general Formula 21:- C6H5CH2O2CCH2CO2A wherein A represents tert-butyl, dibenzyl or trityl, and compounds of the following general Formula 36 (being the combination of Formulae 29 and 35 herein):- wherein X1 represents ethynyl or mono-, di- or trifluoromethyl; R1 is a defined above; R9 represents hydroxy, alkoxy or amino; and R10 represents hydrogen, alkyl, phenylalkyl, phenyl or p-methoxyphenyl.
Inventors:
FUIRITSUPE BEI
BURAIAN UORUTAA METOKAAFU
JIEFURII SUCHIYUWAATO WAIZUMAN
BURAIAN UORUTAA METOKAAFU
JIEFURII SUCHIYUWAATO WAIZUMAN
Application Number:
JP6970880A
Publication Date:
May 23, 1981
Filing Date:
May 27, 1980
Export Citation:
Assignee:
MERRELL TORAUDE & CO
International Classes:
A61K31/40; A61P43/00; C07C59/58; C07C67/00; C07C69/716; C07C229/22; C07C229/34; C07C231/00; C07C233/45; C07C233/47; C07C69/738; C07C233/49; C07C233/51; C07C235/74; C07C237/12; C07C237/20; C07C237/22; C07C239/14; C07C239/20; C07C253/00; C07C255/27; C07C255/41; C07C259/06; C07D205/04; C07D207/16; C07D209/48; C07D211/60; C07D339/08; C07D409/06; C07F7/08; (IPC1-7): A61K31/40; C07C69/738; C07C101/34; C07C103/46; C07C103/49; C07C103/66; C07C103/68; C07C121/417; C07C121/66; C07D207/16