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。
Abstract
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
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Key words
imatinib mesylate /
chronic myeloid leukemia /
synthesis
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李铭东;李东;吉民.
甲磺酸伊马替尼的合成[J]. 中国药学杂志, 2008, 43(03): 228-229
LI Ming-dong;LI Dong;JI Min.
Synthesis of Imatinib Mesylate [J]. Chinese Pharmaceutical Journal, 2008, 43(03): 228-229
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参考文献
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脚注
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