Construction of Quaternary Carbon Center by Catalytic Asymmetric Alkylation of 3‐Arylpiperidin‐2‐ones Under Phase‐Transfer Conditions
作者:Tomoaki Inukai、Taichi Kano、Keiji Maruoka
DOI:10.1002/anie.201913518
日期:2020.2.3
A highly enantioselective synthesis of δ-lactams having a chiral quaternary carbon center at the α-position has been developed through an asymmetric alkylation of 3-arylpiperidin-2-ones underphase-transferconditions. In this transformation, a 2,2-diarylvinyl group on the δ-lactam nitrogen atom plays a crucial role as a novel protecting group and an achiral auxiliary for improving both yield and enantioselectivity
The present invention relates to compound of formula (I) wherein R1, R2, R3, R4, R5, R6, R7, and X are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases, which are associated with the modulation of CB1 receptors.
Spiro-tricyclicaromatic succinimide derivatives as inhibitors of aldose
申请人:Alcon Laboratories, Inc.
公开号:US05153211A1
公开(公告)日:1992-10-06
Disclosed are substituted or unsubstituted planar tricyclic fluorene or nuclear analogs thereof, spiro-coupled to a five-membered ring containing a secondary amide, and the pharmaceutically acceptable salts thereof. These compounds are useful, inter alia in the treatment of diabetes. Also disclosed are processes for the preparation of such compounds; pharmaceutical compositions comprising such compounds; and methods of treatment comprising administering such compounds and compositions when indicated for, inter alia, long term, prophylactic treatment of the diabetes syndrome. A particularly preferred class of compounds comprise difluoro-dialkoxy substituted spiro-(9H-fluorene-9,4'-imidazolidine)-2',5-diones.