Development of a Large Scale Asymmetric Synthesis of Vanilloid Receptor (TRPV1) Antagonist ABT-102

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• 作者：Kirill Lukin ; Margaret C. Hsu ; Gilles Chambournier ; Brian Kotecki ; C. J. Venkatramani ; M. Robert Leanna
• 刊名：Organic Process Research & Development
• 出版年：2007
• 出版时间：May 2007
• 年：2007
• 卷：11
• 期：3
• 页码：578 - 584
• 全文大小：104K
• 年卷期：v.11,no.3(May 2007)
• ISSN：1520-586X

文摘

A highly efficient asymmetric synthesis of TRPV1 antagonistABT-102 was developed and successfully demonstrated on amulti-kilogram scale. This process incorporates a new asymmetric synthesis of (R)-tert-butylaminoindan, which is based ona chiral auxiliary induced diastereoselective reduction of itsiminoindan precursor.