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首页> 外国专利> THIAZOLBENZOHETEROCYCLES, METHODS OF THEIR SYNTHESIS, MEDICINAL AGENT, INTERMEDIATE SUBSTANCES FOR SYNTHESIS OF THIAZOLBENZOHETEROCYCLES

THIAZOLBENZOHETEROCYCLES, METHODS OF THEIR SYNTHESIS, MEDICINAL AGENT, INTERMEDIATE SUBSTANCES FOR SYNTHESIS OF THIAZOLBENZOHETEROCYCLES

机译：噻吩并杂环化合物，其合成方法，药物，中间体，用于合成噻吩并杂环化合物

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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
机译：领域：有机化学，化学技术，药学。物质：本发明涉及通式（I）的新型噻唑苯并杂环。其中R 1 表示硫原子; R 2 表示氢原子; -R 3 -R 4 -R 5 -R 6 -表示公式链：，依此类推; R 7 是指多氟烷基或多氟烷氧基。 R 8 表示羟基; R 9 表示苄基; R 10 表示烷基，-CH 2 OH，-COOMe，-COOH或-CONH 2 ，它们的异构体，外消旋体，对映异构体和与无机或有机酸。本发明还涉及式（I）的化合物的合成方法，其中将碱金属硫氰酸盐或碱金属硒氰酸盐加入到与式（II）的衍生物的反应中。或式（I）的化合物，其中R 2 表示氢原子; -R 3 -R 4 -R 5 -R 6 -表示式为-CH 2 -CH 2 -CH 2 -CH（R 8 ）-和R 8 表示通过还原式（I）的相应化合物合成的羟基，其中R 2 表示氢原子，-R 3 -R 4 -R 5 -R 6 -表示式为-CH 2 -CH 2 -CH 2 -CO-;或式（I）化合物，其中R 2 是氢原子; -R 3 -R 4 -R 5 -R 6 -表示公式链-CH 2 -CH 2 -CH 2 -SO-，-CH 2 -CH 2 - CH 2 -SO 2 -CH 2 -等，是通过氧化相应的式（I）化合物合成的，其中-R 3 -R 4 -R 5 -R 6 -表示式-CH 2的链 -CH 2 -CH 2 -S，-CH 2 -CH 2 -S- CH 2 -。分离合成的化合物，并且如果需要将其转化为盐。本发明还涉及具有抗惊厥作用的药物，其包含式（I）的化合物或其药学上可接受的盐与无机或有机酸以及药学上可接受的载体。本发明还涉及式（II）的衍生物，其中-R 3 -R 4 -R 5 -R 6 -表示式-CH 2 -CH 2 -CH 2 -CH 2 -的链， -CH 2 -CH 2 -CH 2 -S等; R 7 / 是指多氟烷基或多氟烷氧基。 R 8 表示羟基; R 9 表示苄基; R 10 是指烷基，-CH 2 OH，-COOMe，-COOH或-CONH 2 。本发明提供了新的噻唑苯并杂环的合成。效果：改进的合成方法，化合物的重要药用特性。 9厘升，25前

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