ENKEPHALINE ANALOGUE MODULATING BRAIN FUNCTION, ATTENUATING CONVULSIVE REACTION, ACCELERATING CONSOLIDATION AND REPRODUCIBILITY OF INFORMATION UNDER STRESS CONDITIONS

摘要

FIELD: organic chemistry. SUBSTANCE: product: enkephaline analogue of the formula Tyr-DOrn(Ac)-Gly-Phe-OH. Reagent 1: N^{-tert.-butylhydroxycarbonyl-N-benzylhydroxycarbonyl-D-or- nitylglycylphenylalanine trifluoroacetate synthesized from L-phenylalanine. The latter is added to interaction with tret. -butylhydroxycarbonylglycyl in aqueous-alkaline medium in the presence of pentachlorophenyl ester. Formed N-tert.-butylhydroxycarbonylglycylphenylalanine is deblocked, converted to triacetate form and condensed with N-tert. -butylhydroxycarbonyl-N-benzylhydroxycarbonyl-D-or- nitine pentafluorophenyl ester. Reagent 2: N,)-di-Boc-L-tyrosine pentafluorophenyl ester. Process is carried out in dimethylformamide in the presence of N-ethyldiisopropylamine at 0 C and stirring. Condensation product is deblocked and interacted with p-nitrophenylacetate in the presence of N-ethyldiisopropylamine. The yield of the end product is 36% ()D22+67,3, R_f + 67.3 C, Rf value is determined in three systems. Synthesized compound is used in medicine. EFFECT: improved method of synthesis. 3 tbl}