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Synfacts 2011(5): 0468-0468  
DOI: 10.1055/s-0030-1259768
Synthesis of Natural Products and Potential Drugs
© Georg Thieme Verlag Stuttgart ˙ New York

Synthesis of Casopitant

Contributor(s): Philip Kocienski
R. di Fabio et al.*
GlaxoSmithKline Medicines Research Centre, Verona, Italy
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Publication History

Publication Date:
15 April 2011 (online)

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Significance

Casopitant is one of the most potent NK1 receptor antagonists discovered to date. It has been selected as a clinical candidate for the treatment of major depression disorders. The key step in the synthesis depicted is the construction of the 2-arylpiperidin-4-one core via the nucleophilic addition of an aryl Grignard reagent to an N-acylpyridinium salt derived from reaction of A with CbzCl.