Enantioselective, biocatalytic reduction of 3-substituted cyclopentenones: Application to the asymmetric synthesis of an hNK-1 receptor antagonist
A convergent and enantioselective route to the hNK-1 receptor antagonist (1) is described, which sets all six stereogenic centers with high diastereoselectivity and delivers 1 in only 11 steps and 23% overall yield. The process was enabled by the developm
Campos, Kevin R.,Klapars, Artis,Kohmura, Yoshinori,Pollard, David,Ishibashi, Hideaki,Kato, Shinji,Takezawa, Akihiro,Waldman, Jacob H.,Wallace, Debra J.,Chen, Cheng-Yi,Yasuda, Nobuyoshi
p. 1004 - 1007
(2011/05/08)
PROCESS FOR MAKING LACTAM TACHYKININ RECEPTOR ANTAGONISTS
The present invention is directed to a process for preparing certain α,α disubstituted γ-lactam derivatives that are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The compounds are useful i
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Page/Page column 30-31
(2008/06/13)
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