甲磺酸伊马替尼的合成  

Synthesis of imatinib mesylate

作　　者：王保国[1] 刘玉凤[1] 狄国杰[1] 许鹏飞[1] 朱鹏[1] 付茂文[1] 

机构地区：[1]济宁医学院药学院,山东日照276826

出　　处：《济宁医学院学报》2012年第2期103-105,共3页Journal of Jining Medical University

基　　金：济宁医学院2008年青年基金项目

摘　　要：目的研究和改进甲磺酸伊马替尼的合成工艺。方法以3-乙酰吡啶、4-甲基-3-硝基苯胺等为原料,经过环合、氯化、还原、缩合,进而与甲磺酸成盐得到甲磺酸伊马替尼。结果目标化合物经质谱、核磁共振氢谱等确证,总收率45.7%。结论该合成方法简便,成本低,适合工业化生产。Objective To research and improve the synthesis of imatinib mesylate.Methods Using 3-acetylpyridine and 4-methyl-3-nitroaniline as raw matrials,imatinib mesylate was synthesized by cyclization,chlorination,reduction,condensation and salification with methane sulfonic acid.Results The structure of target compound was identified by MS and 1H-NMR.The overall yield was 45.7%.Conclusion The simple cost-saving synthetic method can be used in the industrial preparation.

关 键 词：伊马替尼 合成 酪氨酸激酶抑制剂 

分 类 号：R914.5[医药卫生—药物化学]