Mocetinostat的合成研究  

Study on Process of Synthesizing Mocetinostat

作　　者：刘昭文[1] 郭小华[1] 曾发挥[1] 杨凯[1] LIU Zhao-Wen;GUO Xiao-Hua;ZENG Fa-Hui;YANG Kai(College of Pharmacy Gannan Medical University,Ganzhou 341000,China)

机构地区：[1]赣南医学院药学院

出　　处：《海峡药学》2019年第10期64-66,共3页Strait Pharmaceutical Journal

基　　金：赣南医学院校级课题(No.YB201705)

摘　　要：目的改进组蛋白去乙酰化酶抑制剂Mocetinostat的合成工艺。方法以4-甲基苯甲酸乙酯为起始原料,经溴代,与中间体4-(3-吡啶基)-2-氨基-嘧啶取代,再经水解、缩合、催化氢化制得目标物Mocetinostat。结果Mocetinostat合成总收率为45.4%,纯度99.6%,所得产品经质谱(MS)、核磁共振氢谱(1H-NMR)确证。结论改进后的工艺过程简单,反应条件温和,环境友好,产品收率高,有利于工业化大生产。OBJECTIVE To improve the synthesis process of Histone deacetylase inhibitor Mocetinostat.METHODS Mocetinostat was synthesized from Ethyl 4-methylbenzoate by reaction of bromation、Substituted with intermediate 4-(3-pyridinyl)-2-aminopyridine、hydrolysis、condensation、catalytic hydrogenation.RESULTS The total yield was 45.4%,and the purity was 99.1%.The structure of target compound was confirmed by MS,1H-NMR.CONCLUSION This process had the advantages of simple operation,mild reaction conditions,environment friendly,good yield,and suitable for industrial production.

关 键 词：组蛋白去乙酰化酶抑制剂 4-甲基苯甲酸乙酯 合成 Mocetinostat 

分 类 号：R917[医药卫生—药物分析学]