An Efficient, Practical Approach to the Synthesis of 2,4-Disubstituted Thiazoles and Oxazoles: Application to the Synthesis of GW475151

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• 作者：Stephen A. Hermitage ; Kevin S. Cardwell ; Tim Chapman ; Jason W. B. Cooke ; and Rebecca Newton
• 刊名：Organic Process Research & Development
• 出版年：2001
• 出版时间：January 2001
• 年：2001
• 卷：5
• 期：1
• 页码：37 - 44
• 全文大小：88K
• 年卷期：v.5,no.1(January 2001)
• ISSN：1520-586X

文摘

A new method for the synthesis of 2,4-disubstituted oxazolesand thiazoles and 2,4,5-trisubstituted oxazoles from readilyavailable starting materials is described. The methodology hasbeen applied on multigram scale and involves transfer ofoxidation state through a molecular framework. In particularthe oxazole-containing amino acid fragment of the 5,5-trans-fused lactam GW475151, 1, has been prepared in excellent yieldand purity.