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A new and efficient preparation of 2-aminothiazole-5-carbamides: applications to the synthesis of the anti-cancer drug dasatinib
ARKIVOC Pub Date : 2009-11-25 , DOI: 10.3998/ark.5550190.0011.604
Bang-Chi Chen , Rulin Zhao , Bei Wang , Roberto Droghini , Jean Lajeunesse , Pierre Sirard , Masaki Endo , Balu Balasubramanian , Joel C. Barrish

A new and efficient method has been developed for the synthesis of 2-amino-N-(-(2-chloro-6methylphenyl)-thiazole-5-carboxamide. The new method involves a chemoselective αbromination of β-ethoxyacrylamide followed by a one-pot treatment with thiourea to give the desired 2-aminothiazole-5-carboxylamide in excellent yield. Application of this new method to the efficient synthesis of the anti-cancer drug dasatinib was demonstrated.

中文翻译:

2-氨基噻唑-5-脲的新型高效制备方法:在抗癌药物达沙替尼合成中的应用

已开发出一种新的有效方法来合成 2-氨基-N-(-(2-氯-6 甲基苯基)-噻唑-5-甲酰胺。新方法涉及 β-乙氧基丙烯酰胺的化学选择性 α溴化,然后是单-用硫脲进行锅处理,以优异的收率得到所需的 2-氨基噻唑-5-羧酰胺。证明了这种新方法在抗癌药物达沙替尼的有效合成中的应用。
更新日期:2009-11-25
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