13-(2S)2-AMINO-4-CARBOXYBUTANOYL-1,4,7,10-TETRAOXA-13-AZACY- CLOPENTADECANE HYDROCHLORIDE SHOWING ANTIAMNESIC AND ANTIHYPOXIC EFFECT

摘要

FIELD: heterocyclic compounds. SUBSTANCE: synthesis is carried out by reaction of aza-15-crown-5 with N-carbobenzoxy-L-glutamic acid γ-benzylic ester in dry methylene chloride at -10 C in the presence of dicyclohexylcarbodiimide followed by keeping mixture at 20 C for 12 h. From the mixture 13-(2-benzylhydroxycarbonylamino-4-benzylhydroxycarbonylbutan- oyl)-1,4,7,10-tetraoxa-13-azacyclopentadecane is isolated by column chromatography method which is subjected for hydrogenolysis with hydrogen in the presence of catalyst 10% Pd/C. The yield is 90.5% empirical formula is C₁₅H₂₉ClN₂O₇. Antiamnesic and antihypoxic activities of new compound exceed pyracetam, phenazepam and structure analogue at toxicity LD₅₀ 800 mg/kg. EFFECT: synthesis of new compound with enhanced activity. 3 tbl