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Synfacts 2007(9): 0907-0907  
DOI: 10.1055/s-2007-968830
Synthesis of Natural Products and Potential Drugs
© Georg Thieme Verlag Stuttgart · New York

Synthesis of an LY459477 Intermediate

Contributor(s): Philip Kocienski
D. L. Varie*
Eli Lilly and Co., Indianapolis, USA
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Publication History

Publication Date:
23 August 2007 (online)

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Significance

LY459477 is a glutamate (mGlu2/3) receptor agonist. Starting from precedent provided by Hodgson and co-workers (Tetrahedron 1999, 55, 10815), the Lilly group developed an efficient pilot plant-scale synthesis of the intermediate G en route to LY459477 featuring the desymmetrization of the meso-epoxide D using the chiral dia­mine base E.