甲磺酸伊马替尼的合成 |
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引用本文: | 王保国,刘玉凤,狄国杰,许鹏飞,朱鹏,付茂文. 甲磺酸伊马替尼的合成[J]. 济宁医学院学报, 2012, 35(2): 103-105 |
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作者姓名: | 王保国 刘玉凤 狄国杰 许鹏飞 朱鹏 付茂文 |
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作者单位: | 济宁医学院药学院,山东日照,276826 |
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基金项目: | 济宁医学院2008年青年基金项目 |
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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。
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关 键 词: | 伊马替尼 合成 酪氨酸激酶抑制剂 |
Synthesis of imatinib mesylate |
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Affiliation: | WANG Bao-guo,LIU Yu-feng,DI Guo-jie,et al(Pharmaceutical College,Jining Medical University,Rizhao 276826,China) |
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Abstract: | 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. |
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Keywords: | Imatinib Synthesis Tyrosine kinases inhibitor |
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