PEPTIDES* THEIR ACID SALTS* AND THEIR PREPARATION

摘要

NEW MATERIAL:Peptides of formula I: (R is H or H) and their acid solts. EXAMPLE:(2S, 3R)-3-Amino-2-hydroxy-4-phenyl-butanoyl-(S)-arginine hydrochloride. USE:Anti-inflammatory drugs, carcinostatic improver of Bleomycin. A powerful aminopeptidase B activity. PROCESS:(2S, 3S)-Amino acids of formula II: (X is H; Y is H or amino group) or their reactive derivatives are condensed with (S)-arginine or its derivative having a protected carboxyl and/or guanidino group by the carbodiimide method, etc. to form peptide linkages. In case protective groups are present, the groups are removed by the well-known method and the products are reacted with an acid to give compounds of formula I as reguired. The starting compounds of formula II are obtained by hydrolyzing nitrile delivatives of formula III.