Diarylketone Ketoreductase Screen and Synthesis Demonstration to Access mGlu2 Receptor Potentiators

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• 作者：Nicholas A. Magnus ; D. Scott Coffey ; Amy C. DeBaillie ; Chauncey D. Jones ; Iwona A. Kaluzna ; Spiros Kambourakis ; Yangwei J. Pu ; Lin Wang ; James P. Wepsiec
• 刊名：Organic Process Research & Development
• 出版年：2011
• 出版时间：November 18, 2011
• 年：2011
• 卷：15
• 期：6
• 页码：1377-1381
• 全文大小：751K
• 年卷期：v.15,no.6(November 18, 2011)
• ISSN：1520-586X

文摘

This communication describes proof of concept for an enantioselective enzyme-based synthesis of diarylmethanol (S)-1 to access mGlu2 receptor potentiators. A ketoreductase (KRED) screen was applied to benzophenone 8 to afford chiral diarylmethanol (S)-9, which is a useful intermediate for the preparation of chiral diarylmethanol (S)-1. In addition, a more practical synthesis of benzophenone 8 was demonstrated utilizing Friedel鈥揅rafts acylation and radical bromination chemistry.