Diarylketone Ketoreductase Screen and Synthesis Demonstration to Access mGlu2 Receptor Potentiators

Nicholas A. Magnus, Donald S. Coffey, Amy C. DeBaillie, C. David Jones, Iwona Kaluzna, Spiros Kambourakis, Yangwei John Pu, Lin Wang, James P. Wepsiec

Organic Process Research & Development · 2011 · 12 citations · 7 references

Concepts

Abstract

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–Crafts acylation and radical bromination chemistry.

References

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