Pd(II)-Catalyzed Phosphorylation of Enamido C(sp(2))-H Bonds: A General Route to -Amido-vinylphosphonates

Organophosphorus compounds are essential structures in modern pharmaceutical, agrochemical, and material sciences. The development of new and efficient methods for the synthesis of C-P bonds has been an important focus of research. We herein report a Pd-catalyzed enamido C(sp(2))-H phosphorylation for direct construction of C-P bonds under simple and convenient conditions without the need for additional ligands or directing groups. The present reaction can tolerate a wide range of functional groups, and furnish a variety of phosphorylation products including tetrasubstituted-vinyl -aminophosphonates that are otherwise difficult to access. This protocol was also exemplified into the late-stage modification of bioactive natural products and was suitable for large-scale synthesis.