| 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,(2):103-105 |
| 甲磺酸伊马替尼的合成 |
| Synthesis of imatinib mesylate |
| 投稿时间：2012-03-03 |
| DOI：10.3969/j.issn.10009760.2012.02.006 |
| 中文关键词: 伊马替尼 合成 酪氨酸激酶抑制剂 |
| 英文关键词: Imatinib Synthesis Tyrosine kinases inhibitor |
| 基金项目:济宁医学院2008年青年基金项目 |
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| 中文摘要: |
| 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。 |
| 英文摘要: |
| 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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