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Synfacts 2010(12): 1332-1332  
DOI: 10.1055/s-0030-1258871
Synthesis of Natural Products and Potential Drugs
© Georg Thieme Verlag Stuttgart ˙ New York

Synthesis of BMS-764459

Contributor(s): Philip Kocienski
D. K. Leahy et al.*
Bristol-Myers Squibb Company, New Brunswick and Wallingford, USA
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Publication History

Publication Date:
22 November 2010 (online)

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Significance

Elevated levels of corticotropin-­releasing factor (CRF) are linked to depression, anxiety, and gastrointestinal disorders. BMS-764459 and BMS-763534 are CRF1 antagonists being developed for the treatment of stress. Key steps are a palladium(0)-catalyzed cyanation and an asymmetric Strecker reaction.