| 达沙替尼的合成工艺研究 |
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| 引用本文： | 王 伟,翟 鑫,王 刚,李文韬,宫 平. 达沙替尼的合成工艺研究[J]. 中国药物化学杂志, 2009, 19(1): 36-38 |
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| 作者姓名： | 王 伟 翟 鑫 王 刚 李文韬 宫 平 |
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| 作者单位： | 沈阳药科大学 制药工程学院，辽宁 沈阳 110016 |
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| 摘 要： | 目的 优化酪氨酸激酶抑制剂达沙替尼的合成工艺。方法 以2-氯-6-甲基苯胺为起始原料，经酰胺化、环合、取代、取代共4步反应合成达沙替尼。结果与结论 经4步反应合成达沙替尼，其结构经1H-NMR、MS谱确证。改进后的合成工艺反应条件温和、操作简便，总收率为51.5%。
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| 关 键 词： | 化学合成；酪氨酸激酶抑制剂；达沙替尼 |
| 收稿时间： | 2008-06-17 |
| 修稿时间： | 2008-10-28 |
Study on synthetic process of dasatinib |
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| WANG Wei,ZHAI Xin,WANG Gang,LI Wen-tao,GONG Ping. Study on synthetic process of dasatinib[J]. Chinese Journal of Medicinal Chemistry, 2009, 19(1): 36-38 |
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| Authors: | WANG Wei ZHAI Xin WANG Gang LI Wen-tao GONG Ping |
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| Affiliation: | School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, China |
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| Abstract: | Aim To synthesize dasatinib and optimize its synthetic process. Methods Dasatinib was synthesized from 2-chloro-6-methylaniline via amidation, cyclization, substitution and substitution. Results and conclusion Dasatinib was synthesized in 51.5% yield via four-step sequence and its structure was confirmed by 1H-NMR and MS. The improved process is more practical owing to its advantages of mild conditions. |
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| Keywords: | chemical synthesis tyrosine kinase inhibitors dasatinib |
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