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达沙替尼合成工艺改进 被引量：5

Improvement on the Synthesis of Dasatinib
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摘要 以2-氨基噻唑-5-甲酸甲酯为起始原料,采用一锅法将氨基进行保护并进行甲酯水解,再与2-氯-6-甲基苯胺缩合后,得到的中间体依次与4,6-二氯-2-甲基嘧啶、N-羟乙基哌嗪发生取代反应制得达沙替尼。总收率由原14.9%提高至41.5%,该合成工艺提高了反应收率,降低了生产成本,有利于工业化生产。 Dasatinib was synthesized from methyl 2-amino-thiazole-5-carboxylate in an improved process via 2-chloro-6-methyl aniline as an intermediate in an overall yield of 41.5%,much higher than the usual value of 14.9%.This new process is more suitable for industrial production because of higher yield and lower cost.
作者 安康 关建宁 杨浩 侯雯 万嵘
机构地区 南京工业大学理学院 南京卡文迪许生物工程技术有限公司
出处 《精细化工中间体》 CAS 2011年第2期42-44,共3页 Fine Chemical Intermediates
关键词 达沙替尼 酪氨酸激酶抑制剂 工艺改进 dasatinib tyrosine kinase inhibitor process improvement
分类号 TQ464.51 [化学工程—制药化工]
  • 相关文献

参考文献10

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共引文献34

同被引文献33

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引证文献5

二级引证文献6

精细化工中间体
2011年 第2期

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