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Synfacts 2010(4): 0393-0393  
DOI: 10.1055/s-0029-1219494
Synthesis of Natural Products and Potential Drugs
© Georg Thieme Verlag Stuttgart ˙ New York

Synthesis of a TRPV1 Receptor Antagonist

Contributor(s): Philip Kocienski
S. Yu*, A. Haight, B. Kotecki, L. Wang, K. Lukin, D. R. Hill
Abbott Laboratories, North Chicago, USA
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Publication History

Publication Date:
22 March 2010 (online)

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Significance

The target molecule is a TRPV1 ­receptor antagonist that is being developed for pain management. Noteworthy features of the synthesis are (1) a rare example of a Sonogashira coupling of a chloroarene (A + B → C) and (2) a rare example of the N-arylation of a urea using a chloroarene (E + F → target).