• ezetimibe - 引用次数：2

  -1-(4-fluorophenyl)-3-(3-methoxy-3-oxopropyl)-4-(4-benzyloxyphenyl) -2-azetidinone(20)is an important intermediate of Ezetimibe,based on literature,a commercial and pratical synthesis route with glutaric anhydride as start material was chosen. (20)was prepared by monomethylesterification,chlorination,amidation,imine condensing reaction and cyclizing reaction.

  -1-(4-氟苯基)-3-(3-甲氧基-3-氧代丙基)-4-(4-苄氧基-苯基)-2-氮(杂)环丁酮(20)是依替米贝的重要中间体,本文在查阅大量文献的基础上,选择了戊二酸酐为起始原料的路线进行了详细的研究,经单酯化、酰氯化、酰胺化、亚胺缩合反应、环合反应,最终成功制得了(3R,4S)-1-(4-氟苯基)-3-(3-甲氧基-3-氧代丙基)-4-(4-苄氧基-苯基)-2-氮(杂)环丁酮(20)。

  参考来源 - 依替米贝中间体合成研究

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