| abstract |
A plurality of methods are disclosed for preparing compounds having the formula:n whereinn R is hydrogen, formyl, acetyl, propanoyl, butanoyl, phenylacetyl, phenylpropanoyl, benzoyl, cyclopentanecarbonyl, tert-butyloxycarbonyl, cyclopentanecarbonyl-L-lysyl, pyro-L-glutamyl-L-lysyl, L-lysyl, L-arginyl or pyro-L-glutamyl; A is phenylalanyl, alanyl, tryptophyl, tyrosyl, glycyl isoleucyl, leucyl, histidyl, or valyl, the α-amino group thereof being in amide linkage with R; R 1 is hydrogen or methyl, R2 is L-proline, L-3,4-dehydroproline, D,L-3,4-dehydro- proline, L-3-hydroxyproline, L-4-hydroxyproline, L-thiazo- lidine-4-carboxylic acid, or L-5-oxo-proline, the imino group thereof being in imide linkacge with the adiacentn and, I n is 0 or 1, such that when n is O, R is methyl, and where n= 1 , and R 1 is methyl then moiety is in the D-configuration. These compounds are inhibitors of angiotensin converting enzyme. |