期刊论文

中文

武汉轻工大学学报

2095-7386

2022

41

4

31-34

10.3969/j.issn.2095-7386.2022.04.005

本校为第一机构

对现有的泰泽司他(Tazemetostat)合成工艺进行了改进.以3-氨基-5-溴-2-甲基苯甲酸甲酯为原料,经过两次还原胺化反应,Suzuki偶联,水解,缩合5步反应得到目标化合物泰泽司他(Tazemetostat).结果显示:经1 H-NMR、LC-MS确认为目标化合物,总产率57.6％(以3-氨基-5-溴-2-甲基苯甲酸甲酯计),纯度达99.1％(HPLC法).该方法操作简单,无柱层析操作,收率、纯度高,适合工业化生产.

Objective:To improve the existing synthesis process of Tazemetostat.Methods:The target compound Tazemetostat was obtained from methyl 3-amino-5-bromo-2-methylbenzoate by a 5-step reaction with two reductive amination reactions,Suzuki coupling,hydrolysis and condensation.Results and conclusions:The target compound was confirmed by 1H-NMR and LC-MS in 57.6%yield(based on methyl 3-amino-5-bromo-2-methylbenzoate)and 99.1%purity(HPLC method).The method has simple operation,no column chromatography operation,high yield and high puri...