Nickel-catalyzed enantioselective α-heteroarylation of ketones <i>via</i> C–F bond activation to construct all-carbon quaternary stereocenters
Xiaodong Gu, Kexin Liu, Limin Yang, Chengyi Xie, Mingliang Li, Jun Wang
Abstract
C-F bond activation. A series of ketones and 2-fluoropyridine derivatives with different functional groups proceed well to provide the corresponding products containing all-carbon quaternary stereocenters in good yields (up to 99% yield) and high ee values (up to 99% ee). In addition, drug molecule donepezil could also be compatible under the reaction conditions to afford late-stage diversification of pharmaceuticals.
Topics & Concepts
StereocenterEnantioselective synthesisNickelCatalysisChemistryQuaternary carbonStereochemistryMedicinal chemistryOrganic chemistryFluorine in Organic ChemistryCatalytic C–H Functionalization MethodsCyclopropane Reaction Mechanisms