Palladium-Catalyzed Hydrogenative Kinetic Resolution of Atropisomeric Coumarins

Abstract

Coumarin derivatives are widely utilized in numerous pharmaceutical studies. However, the asymmetric synthesis of coumarins containing axial chirality has remained largely unexplored. In this work, we present a palladium-catalyzed hydrogenative kinetic resolution of atropisomeric coumarins, which exhibits broad substrate compatibility and achieves high enantioselectivity, with the selectivity factor reaching up to 107.4. A gram-scale experiment and enantiomerization barrier determination further demonstrate the practical applicability and robustness of the methodology.