| 引用本文: | 杨照,王志祥,方正,鲍书馨,郭凯.马赛替尼合成工艺研究[J].中国现代应用药学,2013,30(1):35-38. |
| YANG Zhao,WANG Zhixiang,FANG Zheng,BAO Shuxing,GUO Kai.Study on the Synthesis of Masitinib[J].Chin J Mod Appl Pharm(中国现代应用药学),2013,30(1):35-38. |
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| 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。 |
| 关键词: 马赛替尼 合成 抗肿瘤 |
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| 基金项目:国家973课题(2012CB721104) |
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| Study on the Synthesis of Masitinib |
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YANG Zhao1, WANG Zhixiang1, FANG Zheng2, BAO Shuxing2, GUO Kai2
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1.School of Pharmacy, China Pharmaceutical University, Nanjing 210009, China;2.School of Pharmaceutical Science, Nanjing University of Technology, Nanjing 210009, China
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| Abstract: |
| 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. |
| Key words: masitinib synthesis antitumor |
