METHOD OF SYNTHESIS OF PYRANYL-CYANOGUANIDINE DERIVATIVES Russian patent published in 1996 - IPC

FIELD: organic chemistry. SUBSTANCE: products: derivatives of pyranyl-cyanoguanidine of the formula (I) where a, b, c are carbon atoms or one of a, b, c can mean nitrogen and others - carbon atom; R₁ - groups where R₂ - CN; R₃, R₄ - CH₃; R₅ - NO₂, ethynyl, phenylethynyl; R₆ - H; R₇ - C₁-C₈-alkyl, unsubstituted phenyl or phenyl substituted with halogen atom, C₁-C₈-alkyl, haloid-C₁-C₈-alkyl, lower alkoxy-group or amino-group which is substituted with lower alkyl; R₃ - H or CH₃ or R₇ and R₈ together with bound nitrogen atom form pyrrolidine ring; R₉ - H or CH₃. Reagent 1: thiourea of the formula where R₇ and R₈ as indicated above. Reagent 2: amine of the formula (III) where R₂, R₃, R₄, R₅, R₆ and R₉ have values indicated above. Process conditions: in the presence of carbodiimide and acid, in the medium of organic solvent. These compounds show activity with relation to potassium channel activation and can be useful, for example, as cardial-vessel agents, especially as antiischemic agents. Lactic dehydrogenase activity decrease at 10 M - 60%. Synthesized compounds were used in medicine. EFFECT: improved method of synthesis. 1 tbl