Pd-catalyzed enantioselective C–H arylation of phosphinamides with boronic acids for the synthesis of P-stereogenic compounds

Abstract A Pd-catalyzed enantioselective C–H arylation of phosphinamides with aryl boronic acids is presented. With readily affordable amino acid derivatives as chiral ligands, the reaction proceeded efficiently to afford the P-stereogenic phosphinamides in up to 75% yield and with 99% ee under mild conditions. Most importantly, the reaction could be performed on a large scale for various substrates. This method provides an alternative and reliable way for accessing P-stereogenic phosphinamides.