甲磺酸伊马替尼的合成  

Synthesis of Imatinib Mesylate

作　　者：李铭东[1] 李东[2] 吉民[1] 

机构地区：[1]东南大学化学化工学院,东南大学制药工程研究所,南京210096 [2]东南大学附属南京江北人民医院,南京210048

出　　处：《中国药学杂志》2008年第3期228-229,共2页Chinese Pharmaceutical Journal

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、2-甲基-5-硝基苯胺等为原料,经缩合、成环、氢化、酰化,进而与甲磺酸成盐得到甲磺酸伊马替尼。结果中间体及目标化合物经质谱、核磁共振氢谱、红外光谱等确证,总收率27.0%。结论本路线操作简单,成本较低,适合工业化生产。OBJECTIVE To study and improve the synthesis of imatinib mesylate. METHODS Imatinib mesylate was prepared from 1-（pyridine-3-yl） ethanone and 2-methyl-5-nitrobenzenamine by condensation, cyclization, hydrogenation, acylation and salification with methane sulfonic acid. RESULTS The structure of target compound was identified by MS and ^1H-NMR. The overall yield was 27.0%. CONCLUSION This cost-saving and simplified method can be used in the industrial preparation.

关 键 词：甲磺酸伊马替尼 慢性髓细胞白血病 合成 

分 类 号：R914.5[医药卫生—药物化学]