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| 伊马替尼的合成及其中间体工艺优化 | |
| 引用本文： | 罗忠枚,魏玮,夏小冬,曹胜华,丁小东. 伊马替尼的合成及其中间体工艺优化[J]. 化学研究与应用, 2012, 24(3): 484-487 |
| 作者姓名： | 罗忠枚 魏玮 夏小冬 曹胜华 丁小东 |
| 作者单位： | 1. 中国医药集团总公司 四川抗菌素工业研究所,四川成都,610052 2. 四川大学分析测试中心,四川成都,610064 |
| 摘 要： | 以3-乙酰基吡啶为起始原料,经环合、缩合、还原、酰胺化等六步反应制得抗肿瘤药物伊马替尼,并对其中间体N-(2-甲基-5-硝基苯基)-4-(3-吡啶基)嘧啶-2-胺的后处理工艺进行了优化,降低了成本和操作难度,有利于工业化。 |
| 关 键 词： | 3-乙酰基吡啶 伊马替尼 工艺优化 |
Synthesis of imatinib and the optimization of its intermediat |
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| LUO Zhong-mei , WEI Wei , XIA Xiao-dong , CAO Sheng-hua , DING Xiao-dong. Synthesis of imatinib and the optimization of its intermediat[J]. Chemical Research and Application, 2012, 24(3): 484-487 | |
| Authors: | LUO Zhong-mei WEI Wei XIA Xiao-dong CAO Sheng-hua DING Xiao-dong |
| Affiliation: | 1.Sichuan Industrial Institute of Antibiotics,China National Pharmaceutical Group Corporation,Chengdu 610052,china; 2.Analytical & Testing Center,Sichuan University,Chengdu 610064,China) |
| Abstract: | The anti-cancer drug imatinib was synthesized through six main reactions such as cyclization,condensation,reduction and amidation etc.The after-treatment of N-(2-methyl-5-nitrophenyl)-4-(pyridine-3-yl)pyrimidin-2-amine,the intermediate of imatinib,was optimized greatly.The improved after-treatment method featured with low cost,easy operation procedure and could be readily scale-up to mass production. |
| Keywords: | 3-acetylpyridine imatinib process optimization |
| 本文献已被 CNKI 万方数据 等数据库收录！ | |