Attrition-Enhanced Deracemization in the Synthesis of Clopidogrel - A Practical Application of a New Discovery

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• 作者：Maarten W. van der Meijden ; Michel Leeman ; Edith Gelens ; Wim L. Noorduin ; Hugo Meekes ; Willem J. P. van Enckevort ; Bernard Kaptein ; Elias Vlieg ; Richard M. Kellogg
• 刊名：Organic Process Research & Development
• 出版年：2009
• 出版时间：November 20, 2009
• 年：2009
• 卷：13
• 期：6
• 页码：1195-1198
• 全文大小：116K
• 年卷期：v.13,no.6(November 20, 2009)
• ISSN：1520-586X

文摘

The recently discovered technique of deracemization by means of attrition-induced grinding of a solid conglomerate in contact with a solution wherein racemization occurs has been used with a derivative of 2-chlorophenyl glycine, the key chiral component in the synthesis of Clopidogrel (Plavix). Deracemization of the racemate proceeds to a single enantiomer and in essentially absolute enantiomeric excess. Further conversion of enantiomerically pure material to Clopidogrel was achieved in 88% yield.