Practical Synthesis of 2-Amino-5-fluorothiazole Hydrochloride

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• 作者：Paul H. Briner ; Matthew C. T. Fyfe ; Pierre Martin ; P. John Murray ; Fr&eacute ; d&eacute ; ric Naud ; and ; and Martin J. Procter
• 刊名：Organic Process Research & Development
• 出版年：2006
• 出版时间：March 2006
• 年：2006
• 卷：10
• 期：2
• 页码：346 - 348
• 全文大小：32K
• 年卷期：v.10,no.2(March 2006)
• ISSN：1520-586X

文摘

The first synthesis of 2-amino-5-fluorothiazole hydrochlorideis reported from 2-aminothiazole. The synthesis proceeds in35% overall yield, involves no chromatographic purification,and has been employed to prepare multikilogram quantities ofthe title compound. The key fluorine-introducing step comprisesthe reaction of dilithiated 2-tert-butoxycarbonylaminothiazolewith N-fluorobenzenesulfonimide.