马赛替尼合成工艺研究  

Study on the Synthesis of Masitinib

作　　者：杨照[1] 王志祥[1] 方正[2] 鲍书馨[2] 郭凯[2] 

机构地区：[1]中国药科大学药学院,南京210009 [2]南京工业大学药学院,南京210009

出　　处：《中国现代应用药学》2013年第1期35-38,共4页Chinese Journal of Modern Applied Pharmacy

基　　金：国家973课题(2012CB721104)

摘　　要：目的改进抗肿瘤药马赛替尼(1)的合成工艺。方法以2-甲基-5-硝基苯胺为原料,与硫氰酸铵和乙酰氯的反应产物发生加成反应得硫脲化合物5,5与自制的2-溴-1-(吡啶-3-基)乙酮氢溴酸盐(2)环合成噻唑化合物6,6还原后与自制的酰氯化合物3反应成酰胺得马赛替尼(1)。结果总收率为28.0%(以2-甲基-5-硝基苯胺计),各步关键中间体及目标物结构经MS和1H NMR确证。结论改进后的方法简化了操作,降低了成本,适合于工业化生产。OBJECTIVE To improve the synthesis process of the anticancer drug Masitinib.METHODS Masitinib(1) was synthesized using 2-methyl-5-nitroaniline as the starting material,via addition,cyclization with self-made compound 2,reduction,and amidation with acyl chloride compound 3.RESULTS The total yield was 28.0% basing on the row material 2-methyl-5-nitroaniline and structures of the key intermediates and the target were confirmed by MS and 1H NMR.CONCLUSION Compared with the literature method,the improved process has the advantages of low-cost,convenient operation and broad prospects for commercial scale-up.

关 键 词：马赛替尼 合成 抗肿瘤 

分 类 号：TQ461[化学工程—制药化工] R914[医药卫生—药物化学]