Download PDF
Synfacts 2010(3): 0253-0253  
DOI: 10.1055/s-0029-1219297
Synthesis of Natural Products and Potential Drugs
© Georg Thieme Verlag Stuttgart ˙ New York

Synthesis of the NK1 Receptor Antagonist GW597599

Contributor(s): Philip Kocienski
G. Guercio*, S. Bacchi et al.*
GlaxoSmithKline Medicines Research Center, Verona, Italy; Sanofi-Aventis R&D Centre, Toulouse and Pharmasynthese, Saint Pierre lès Elbeuf, France
Further Information

Publication History

Publication Date:
18 February 2010 (online)

    Permissions and Reprints

Significance

GW597599 is an NK1 receptor ­antagonist being developed for the treatment of chemotherapy-induced emesis. Noteworthy features are (a) the easy epimerization of the Schiff base derived from E thereby enabling a crystallization-induced diastereoselection and (b) a synthesis of the carbamoyl chloride J that avoids the use of triphosgene.