CAS: 86347-12-8; 1-(2,3-Dimethylphenyl)-1-(1H-Imidazol-4-yl)Ethanol

相似化合物

128366-50-7 86347-14-0 1587636-55-2

📜2,3-二甲基溴苯置于magnesium,1,2-二溴乙烷体系中,用 四氢呋喃 作为反应溶剂,化学反应 8.0H,反应生成 1-(2,3-二甲基苯基)-1-(1H-咪唑基-4-基)乙醇
参考文献: Method For Preparing Dexmedetomidine[fr] Procédé De Préparation De Dexmédétomidine
标题: Method For Preparing Dexmedetomidine[fr] Procédé De Préparation De Dexmédétomidine
摘要:本发明涉及一种制备具有以下结构式(I)的地西泮的方法,或其药学上可接受的盐和/或溶剂化物,包括以下连续步骤:A)不对称氢化以下结构式(II)的亚甲基衍生物,以获得地西泮,并b)选择性地将地西泮盐化和/或溶剂化,以获得地西泮的药学上可接受的盐和/或溶剂化物,其中结构式(II)的亚甲基衍生物是由以下结构式(V)的卤化物和以下结构式(Vi)的氰基咪唑制备而成.本发明还涉及从结构式(V)的卤化物和结构式(Vi)的氰基咪唑制备地西泮合成中间体的方法,这些合成中间体是结构式(II)的亚甲基衍生物,以下结构式(Iii)的醇和以下结构式(Iv)的酮.

专利信息

专利号:US-11718586-B2
优先权日:2019-11-08
标 题:Method for preparing dexmedetomidine
发明人：DIKER KHALID; GORINS GILLES; OZANNE-BEAUDENON AURÉLIE; GOLDSTEIN CORINNE
权利人:NORCHIM
摘要:The present invention relates to a method for preparing dexmedetomidine having the following formula (I): or a pharmaceutically acceptable salt and/or solvate thereof, comprising the following successive steps: a) asymmetric hydrogenation of a methylene derivative of the following formula (II): in order to obtain dexmedetomidine, and b) optionally salifying and/or solvating dexmedetomidine in order to obtain a pharmaceutically acceptable salt and/or solvate of dexmedetomidine, wherein the methylene derivative of formula (II) is prepared from a halide of the following formula (V), in which Hal 2 represents a halogen atom such as Br, and a cyanoimidazole of the following formula (VI). The present invention relates also to methods for preparing synthesis intermediates of dexmedetomidine from the halide of formula (V) and the cyanoimidazole of formula (VI), these synthesis intermediates being the methylene derivative of formula (II), an alcohol of the following formula (III), and a ketone of the following formula (IV).