| 达沙替尼的合成研究 |
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| 引用本文： | 黄睿,何小兵,陈中豪,熊远珍.达沙替尼的合成研究[J].化学与生物工程,2013(10):48-50. |
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| 作者姓名： | 黄睿 何小兵 陈中豪 熊远珍 |
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| 作者单位： | 南昌大学药学院,江西南昌330001 |
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| 摘 要： | 以2-氯-6-甲基苯胺为起始原料,在吡啶的催化下,以99％的转化率得到酰化产物（E）-N-（2-氯-6-甲基苯基）-3-乙氧基丙烯酰胺（Ⅲ）;Ⅲ在以水为主的溶剂中与N-溴代丁二酰亚胺（NBS）、硫脲经“一锅法”连续反应得化合物2-氨基-N-（2-氯-6-甲基苯基）-5-噻唑甲酰胺（V）;V经纯化后与4,6-二氯-2-甲基嘧啶反应得化合物2-（6-氯-2-甲基嘧啶-4-氨基）-N-（2-氯-6-甲基苯基）-5-噻唑甲酰胺（Ⅵ）;Ⅵ与1-（2-羟乙基）哌嗪缩舍得达沙替尼（Ⅶ）,总收率为71％.该合成方法条件温和、反应步骤少、收率高.
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| 关 键 词： | 达沙替尼 酪氨酸激酶抑制剂 合成 |
Study on Synthesis of Dasatinib |
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| HUANG Rui,HE Xiao-bing,CHEN Zhong-hao,XIONG Yuan-zhen.Study on Synthesis of Dasatinib[J].Chemistry & Bioengineering,2013(10):48-50. |
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| Authors: | HUANG Rui HE Xiao-bing CHEN Zhong-hao XIONG Yuan-zhen |
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| Affiliation: | (College of Pharmacy, Nanchang University, Nanchang 330001, China) |
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| Abstract: | Catalyzed by pyridine, compound IT was synthesized by using 2-chloro-6-methyl aniline as raw material with a yield of 99%. Compound V was synthesized from compound Ill and NBS,thiourea in ＂one-pot＂ by using water as main solvent. Compound VI was obtained by compound V and 4,6-dichloride-2-methyl py- rimidine. And then dasatinib was synthesized from condensation reaction of compound and 1-（2-hydroxyeth- yl）piperazine with total yield of 71%. This synthetic method has advantages such as moderate conditions,less reaction step, high yield. |
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| Keywords: | dasatinib tyrosinase kinase inhibitor~ synthesis |
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