Kevin R Campos,
Artis Klapars,
Yoshinori Kohmura,
David Pollard, Hideaki Ishibashi,
Shinji Kato,
Akihiro Takezawa,
Jacob H Waldman,
Debra J Wallace,
Cheng-yi Chen,
Nobuyoshi Yasuda
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ABSTRACT: 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 development of the enantioselective enzymatic reduction of 3-functionalized cyclopentenones and stereospecific Pd-catalyzed etherification coupling of fragments 6 and 7.
Organic Letters 02/2011; 13(5):1004-7. · 5.86 Impact Factor
