Directed C(sp3)‑H Arylation of Free α‑Aminophosphonates: Dual Models Exploration via Palladium Catalysis

In this report, we present the dual activation models for transient directing group-directed and amino-self-directed Pd-catalyzed α-aminophosphonate side-chain C­(sp3)-H arylation. Both strategies showed facile, efficient, and single regioselectivity in the reaction between free α-aminophosphonates and aryl iodides. Furthermore, the modification of amino and late-stage functionalization of the C­(sp3)-P bond from products indicates potential applications for α-aminophosphonates.