Organocatalytic
Kinetic Resolution of Sulfoximines
Shunxi Dong
Marcus Frings
Hanchao Cheng
Jian Wen
Duo Zhang
Gerhard Raabe
Carsten Bolm
10.1021/jacs.6b00143.s002
https://acs.figshare.com/articles/dataset/Organocatalytic_Kinetic_Resolution_of_Sulfoximines/2077960
An
efficient kinetic resolution of sulfoximines with enals was realized
using chiral <i>N</i>-heterocyclic carbene (NHC) catalysts.
The stereoselective amidation proceeds without additional acyl transfer
agent. Both enantiomers of the sulfoximines can be obtained with excellent
ee values (up to 99% ee and −97% ee, respectively). Performing
the catalysis on a gram scale allowed using the recovered sulfoximine
(+)-<b>1j</b> in an asymmetric synthesis of FXa inhibitor <b>F</b>.
2016-02-04 00:00:00
sulfoximine
gram scale
NHC
acyl transfer agent
FXa inhibitor F
Organocatalytic Kinetic Resolution
stereoselective amidation proceeds
ee values