甲磺酸伊马替尼的合成

Synthesis of imatinib mesylate

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.