Synthesis of NK1 Antagonists

O. Dirat; J. M. Elliott; R. A. Jelley; A. B. Jones; M. Reader

doi:10.1055/s-2006-941827

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Synfacts 2006(7): 0647-0647
DOI: 10.1055/s-2006-941827

Synthesis of Natural Products and Potential Drugs

Synthesis of NK₁ Antagonists

Contributor(s): Philip Kocienski
O. Dirat*, J. M. Elliott, R. A. Jelley, A. B. Jones, M. Reader
Merck Sharp and Dohme Research Laboratories, Harlow, UK

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Publikationsverlauf

Publikationsdatum:
22. Juni 2006 (online)

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Significance

The target compound H is a potent neurokinin-1 receptor antagonist intended for the treatment of chemotherapy-induced emesis. The prime feature of the synthesis is the Pd(0)-catalyzed Buchwald α-arylation of the sodium enolate derived from A which delivered B in 100 gram quantities.