Kinetic Resolution of Biaryl Alkenes via Copper-Catalyzed Asymmetric Hydroamination

A highly efficient kinetic resolution of racemic axially chiral biaryl alkenes via the copper-catalyzed asymmetric hydroamination has been developed. This method provides an efficient access to two distinct axial/planar chiral skeletons with high selectivity factors (up to 1057) and exhibits good functional group tolerance, high levels of region- and stereoselectivity (up to 99% ee, >20:1 dr). Moreover, the practical utility of this protocol is demonstrated through gram-scale synthesis and facile post-functionalization, representing the application of asymmetric hydroamination in the kinetic resolution.