Pd-Catalyzed Enantioselective Double C–H Activation and Transmetalation: Synthesis of 2-Heteroaryl/aryl-Ferrocenealdehydes

Synthesis of heterocycle-derived chiral ferrocene formaldehydes opens a new avenue for planar chiral ligands, catalysts, and chiral materials. Herein, PdII/MPAA catalyzed enantioselective double C–H activation, an arylation-oxidative deamination strategy, leads to a step-economical synthetic route for regioselective, monoselective, and enantioselective new heterocycle-substituted chiral ferrocene formaldehydes. The developed methodology is quite general to provide indolizinyl, indolyl, pyrrolyl, furanyl, thiophenyl, oxazolyl, thiazolyl, and aryl-substituted platform ferrocene formaldehydes with up to 60% yield and 97:3 er.