Stereoselective synthesis of 2-amino-3-fluoro bicyclo[3.1.0]hexane-2,6-dicarboxylic acid

Add time:07/26/2019    Source:sciencedirect.com

(+)-2-Aminobicyclo[3.1.0]hexane-2,6-dicarboxylic acid (LY354740) is a conformationally restricted glutamate analogue that is a potent, selective and orally active group 2 metabotropic glutamate receptor agonist possessing anticonvulsant and anxiolytic properties. Herein, we describe a stereoselective and highly efficient synthesis of its 3-beta fluoro derivative using the Corey–Link methodology to create the amino acid stereogenic center.

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