Download PDF
Synfacts 2010(2): 0133-0133  
DOI: 10.1055/s-0029-1219025
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
Further Information

Publication History

Publication Date:
21 January 2010 (online)

    Permissions and Reprints

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 Pd-catalyzed asymmetric vicinal diamination of alkene A using di-tert-butyldiaziridinone B and the phosphoramidite C to give the imidazolidinone D.