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Synfacts 2010(3): 0257-0257  
DOI: 10.1055/s-0029-1219295
Synthesis of Natural Products and Potential Drugs
© Georg Thieme Verlag Stuttgart ˙ New York

Synthesis of Substance P Receptor Antagonist (+)-CP-99,994

Contributor(s): Philip Kocienski
R. Fu, B. Zhao, Y. Shi*
Colorado State University, Fort Collins, USA
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Publication History

Publication Date:
18 February 2010 (online)

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Significance

The binding of the undecapeptide substance P to neurokinin-1 is closely related to the transmission of pain and the induction of neuroinflammatory responses. Substance P antagonists are candidates for the treatment of arthritis, asthma, and migraines. The key step in the synthesis of CP-99,994 is the palladium-catalyzed asymmetric vicinal diamination of alkene A using di-tert-butyldiaziridinone B and the phosphor­amidite C to give the imidazolidinone D.