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Synfacts 2010(12): 1337-1337  
DOI: 10.1055/s-0030-1258869
Synthesis of Natural Products and Potential Drugs
© Georg Thieme Verlag Stuttgart ˙ New York

Synthesis of Telcagepant

Contributor(s): Philip Kocienski
D. P. Steinhuebel*, S. W. Krska*, A. Alorati, J. M. Baxter, K. Belyk, B. Bishop, M. Palucki, Y. Sun, I. W. Davies
Merck & Co., Rahway, USA; Merck Sharp & Dohme Laboratories, Hoddesdon, UK
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Publication History

Publication Date:
22 November 2010 (online)

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Significance

A new, general catalytic asymmetric hydrogenation of allylic amines has been applied to the large-scale synthesis of telcagepant, a drug currently in phase III clinical trials for the treatment of migraine. The reaction uses a cat­ionic ruthenium complex together with the axially chiral ligand (-)-TMBTP.