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Synfacts 2008(3): 0223-0223  
DOI: 10.1055/s-2008-1042664
Synthesis of Natural Products and Potential Drugs
© Georg Thieme Verlag Stuttgart · New York

Synthesis of an NK-1 Receptor Antagonist (CF-17,493)

Contributor(s): Philip Kocienski
S. Caron*, N. M. Do, J. E. Sieser, P. Arpin, E. Vazquez
Pfizer Global R & D, Groton, USA
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Publikationsdatum:
21. Februar 2008 (online)

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Significance

Neurokinin-1 (NK-1) is a small peptide that is upregulated in arthritis, migraine, inflammatory bowel disease, asthma, pain and depression. NK-1 antagonists are potential treatments for these conditions. The synthesis depicted features a nucleophilic trifluoromethylation (A→C) catalyzed by the cinchonine-derived quaternary ammonium fluoride B. For related reactions, see: Tetrahedron Lett. 1994, 35, 3137; Chem. Lett. 2007, 36, 666; Org. Lett. 2007, 9, 3707.