| 摘要 |
FIELD: organic chemistry, chemical technology, pharmacy. SUBSTANCE: invention relates to novel thiazolbenzoheterocycles of the general formula (I) where R1 means sulfur atom; R2 means hydrogen atom; -R3-R4-R5-R6- means chain of formulas: and so on; R7 means polyfluoroalkyl or polyfluoroalk-oxy-group; R8 means hydroxyl; R9 means benzyl; R10 means alkyl, -CH2OH, -COOMe, -COOH or -CONH2, their isomers, racemates, enantiomers and salts with inorganic or organic acid. Invention relates also to method of synthesis of compounds of the formula (I) where alkaline metal thiocyanate or alkaline metal selenocyanate is added to reaction with derivative of the formula (II) or compound of the formula (I) where R2 means hydrogen atom; -R3-R4-R5-R6- means chain of the formula -CH2-CH2-CH2-CH(R8)- and R8 means hydroxyl which are synthesized by reduction of corresponding compound of the formula (I) where R2 means hydrogen atom and -R3-R4-R5-R6- means chain of the formula -CH2-CH2-CH2-CO-; or compound of the formula (I) where R2 means hydrogen atom; -R3-R4-R5-R6- means chain of formulas -CH2-CH2-CH2-SO-,-CH2-CH2-CH2-SO2-CH2- and so on which are synthesized by oxidation of corresponding compound of the formula (I) where -R3-R4-R5-R6- means chain of the formulas -CH2-CH2-CH2-S,-CH2-CH2-S-CH2-. Synthesized compound is isolated and converted to salt if necessary. Invention relates also to medicinal agent eliciting anticonvulsant effect containing compound of the formula (I) or its pharmaceutically acceptable salt with inorganic or organic acid and pharmaceutically acceptable carrier. Invention relates also to derivative of the formula (II) where -R3-R4-R5-R6- means chain of the formulas -CH2-CH2-CH2-CH2-,-CH2-CH2-CH2-S and so on; R7/ means polyfluoroalkyl or polyfluoroalkoxy-group; R8 means hydroxyl; R9 means benzyl; R10 means alkyl, -CH2OH, -COOMe, -COOH or -CONH2. Invention provides synthesis of new thiazolbenzoheterocycles. EFFECT: improved methods of synthesis, valuable medicinal properties of compounds. 9 cl, 25 ex |
