| abstract |
Compounds of the formula :. wherein R is hydrogen, t-butyloxycarbonyl, cyclopentanecarbonyl-L-lysyl, pyro-L-glutamyl-Ij-lysyl, t-lysyl, L-arginyl, pyro-L-glutamyl or R ', wherein R' is formyl, acetyl, propanoyl, butanoyl, phenylacetyl, phenylpropanoyl, benzoyl or cyclopentanecarbonyl; A is phenylalanyl, alanyl, tryptophil, tyrosyl, glycyl, isoleucyl, leucyl, histidyl or valyl, the α-amino group therein being in amide bond with R; R 1 is hydrogen or methyl; n is 0 or 1, so that when n is 0, R is methyl, and when n is 1 and R is methyl, the group in the D configuration is; and R is L-prolyl, L-3,4-dehydroprolyl, L-3-hydroxyprolyl, k-4-hydroxyprolyl, Thiazolidine-4-carboxylic acid or L-5-oxoprolyl, the amino group therein being in bond with the adjacent 0 is prepared by (A) coupling a compound of the formula: ■ in -C-; wherein R . wherein R 1 is either the same as above, or R 2 as above. containing a carbonyl protecting group; (B) removing the R protecting group from the product of step (A), (C) criBetting the product of step (B) with an R-coupling compound wherein R has the meaning given above, and, if necessary, removal of the carbonyl protecting group. The compound of formula (I) are inhibitors of angiotensin-forming enzymes. |