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Synfacts 2010(3): 0257-0257
DOI: 10.1055/s-0029-1219295
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
R. Fu, B. Zhao, Y. Shi*
Colorado State University, Fort Collins, USA
Further Information
Publication History
Publication Date:
18 February 2010 (online)
![](https://www.thieme-connect.de/media/synfacts/201003/lookinside/thumbnails/10.1055-s-0029-1219295-1.jpg)
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.