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Synfacts 2010(4): 0385-0385  
DOI: 10.1055/s-0029-1219487
Synthesis of Natural Products and Potential Drugs
© Georg Thieme Verlag Stuttgart ˙ New York

Synthesis of PF-1247324, a NaV1.8 Sodium Channel Modulator

Contributor(s): Philip Kocienski
M. J. Fray*, A.T. Gillmore, M. S. Glossop, D. J. McManus, I. B. Moses, C. F. B. Praquin, K. A. Reeves, L. R. Thompson*
Pfizer Global Research and Development, Sandwich, UK
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Publication History

Publication Date:
22 March 2010 (online)

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Significance

PF-1247324 is a NaV1.8 sodium channel modulator being developed as a pain therapeutic. Two steps in the kilo-scale synthesis depicted required extensive optimization: (1) the permanganate oxidation of B and (2) the Suzuki-Miyaura coupling of D and E to give biaryl F.