DIPEPTIDE DERIVATIVES OR THEIR PHARMACEUTICALLY ACCEPTABLE SALTS, METHODS OF THEIR SYNTHESIS, ANTIHYPERTENSIVE PHARMACEUTICAL COMPOSITION Russian patent published in 1997 - IPC

FIELD: organic chemistry. SUBSTANCE: products: dipeptide derivatives of the general formula (I): including tautomeric forms where n = 0 or 1; R - halogen, OH, SH, SR₄,OR₄ where R₄ - lower alkyl or phenyl, R₄ NHR₃ where R₅ - phenyl or acetyl, di-(lower alkyl)-amino, COOH or COO-(lower)-alkyl; R₁ - OH, (lower)-alkoxyl; R₂ - lower alkyl; R₃ - halogen, NO₂, (lower)-alkyl, aryl-(lower)-alkyl or their pharmaceutically acceptable salts. Invention proposes two variants of their synthesis: A) by interaction of compound of the formula (II): with dipeptide of the formula (III): in the presence of N₁N-dicyclohexylcarbodiimide followed by if necessary conversion of compound (I) where R - Cl to compound (I) where R - SH and if necessary by hydrolysis, salt formation of esters and diesters synthesized by this manner; B) by interaction of compound (II): where X - halogen and the other values as indicated above except for R - SH with dipeptide (III). Process is carried out in the presence of an organic base; if R₁ - OH then in the presence of inorganic base and if necessary followed by conversion of compound (I) where R - Cl to compound (I) where R - SH and if necessary by hydrolysis and/or salt formation or free acids synthesized by this manner. Antihypertensive pharmaceutical composition has an active component (I) at effective amount. The synthesized compounds were used in medicine for hypertension treatment. EFFECT: improved method of synthesis. 10 cl, 4 tbl