This work pioneers a palladium-catalyzed asymmetric tandem process merging intramolecular C–H arylation with intermolecular Buchwald–Hartwig amination. It establishes the first metal-catalyzed asymmetric synthesis of C–N axially chiral diarylamines, concurrently constructing planar chiral ferrocenes in a single step with high efficiency and stereoselectivity (up to 98% ee, >20:1 d.r.). Mechanistic studies support a sequential pathway where asymmetric C–H arylation generates planar chirality, followed by axial chirality construction via asymmetric C–N coupling.
Gao et al. (Sun,) studied this question.