Easily accessible benzamide-derived P,O ligands (Bphos) for palladium-catalyzed carbon-nitrogen bond-forming reactions.

Easily accessible benzamide-derived hemilabile phosphine ligands were efficiently prepared through ortho-directed lithiation of the corresponding N,N-diethylbenzamide followed by quenching with chlorodialkylphosphines. These structurally simple hemilabile ligands were found to be highly effective in palladium-catalyzed amination of aryl and heteroaryl chlorides. Various sterically congested and functionalized aryl halide substrates were compatible in these reaction conditions.