L-PROLINE DERIVATIVES HAVING ANTIHYPERTENSIVE PROPERTIES AND PROCESS FOR THE PREPARATION THEREOF

摘要

There are described novel angiotensin converting enzyme inhibitors having the general formula: CHEM wherein R represents hydrogen or a formyl, acetyl, propanoyl, butanoyl, phenylacetyl, phenylpropanoyl, benzoyl, cyclopentylcarbonyl, tert-butyloxycarbonyl, cyclopentylcarbonyl-L-lysyl, pyro-L-glutamyl-L-lysyl, L-arginyl, L-lysyl or pyro-L-glutamyl group; A represents a L-phenylalanyl, glycyl, L-alanyl, L-tryptophyl, L-tyrosyl, L-isoleucyl, L-leucyl, L-histidyl or L-valyl group, the alpha -amino group thereof being in amide linkage with R; F1 represents hydrogen or methyl; R2 represents L-proline, L-3,4-dehydroproline, D,L-3,4-dehydroproline, L-3-hydroxyproline, L-4-hydroxyproline or L-thiazolidine, the imino group thereof being in imide linkage with the adjacent -@-; and n is 0 or 1, such that when n=O, R1 represents methyl. The preparation of these compounds is also described. They are useful as orally effective anti-hypertensive agents.