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Synfacts 2009(2): 0119-0119  
DOI: 10.1055/s-0028-1087613
Synthesis of Natural Products and Potential Drugs
© Georg Thieme Verlag Stuttgart ˙ New York

Synthesis of Telcagepant (MK-0974)

Contributor(s): Philip Kocienski
C. S. Burgey*, D. V. Paone, A. W. Shaw, J. Z. Deng, D. N. Nguyen, C. M. Potteiger, S. L. Graham, J. P. Vacca, T. M. Williams
Merck Research Laboratories, West Point, USA
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Publikationsdatum:
22. Januar 2009 (online)

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Significance

Telcagepant is a candidate for the treatment of migraine because it antagonizes the calcitonin gene-related peptide (CGRP) receptor. The synthesis depicted (one of two reported) uses a rhodium-catalyzed Hayashi-Miyaura conjugate addition of an arylboronic acid to a nitroolefin as a key step. The synthesis produced multigram quantities of the target for clinical evaluation.