Synthesis of 4-trifluoromethylated 2-alkyl- and 2,3-dialkyl-substituted azetidines.
[reaction: see text]. A diastereoselective approach to the synthesis of 4-trifluoromethylated 2-alkyl- and 2,3-dialkylazetidines, including BOC-protected 4-trifluoromethylazetidin-2-ylcarboxylic acid, was developed via Wittig reaction of 4-trifluomethylated beta-lactam followed by alkylation and hydrogenation.
Department of Medicinal Chemistry, Merck Research Laboratory, P.O. Box 2000, Rahway, New Jersey 07065, USA. jinlong_jiang@merck.com
Jinlong
J
Jiang
Hemal
H
Shah
Robert J
RJ
DeVita