TRIPEPTIDE DERIVATIVES AS R- OR RS-FORMS OR THEIR PHARMACEUTICALLY ACCEPTABLE NONTOXIC SALTS, PHARMACEUTICAL COMPOSITION Russian patent published in 1997 - IPC

FIELD: organic chemistry, peptides. SUBSTANCE: product: tripeptide derivatives of the general formula: A-Pro-Arg-aldehyde; A - RR, BC; R - free or substituted phenyl, thienyl, free or substituted naphthyl, cyclohexyl; R₁ - hydrogen, lower alkyl, β-lower alkyl, lower alkoxy, or N-(R₂)(R₃) where R₂ and R₃ means independently: hydrogen or lower alkyl; or R₂ - hydrogen and R₃ - acetyl or N - Boc(lower) alkyl; A - bicyclic group, 1,2,3,4-tetrahydroisoquinoline-1- (or 3-)-yl-carbonyl; D - perhydroisoquinoline-1-yl-carbonyl, or their pharmaceutically acceptable nontoxic salts. Reagent 1: APro-OH. Reagent 2: C-protected arginine lactam as trifluoroacetate. Process is carried out in dimethylformamide at -15 C in the presence of N-methylmorpholine for 4 h followed by (for 24 h) slow heating to the room temperature and the synthesized lactam is reduced with methylaluminium hydride. Synthesized compounds inhibit thrombin and can be used in medicine and biochemistry. EFFECT: improved method of synthesis. 14 cl, 4 tbl