Palladium-Catalyzed Enantioselective C–H Activation of Aliphatic Amines Using Chiral Anionic BINOL-Phosphoric Acid Ligands

The design of an enantioselective Pd­(II)-catalyzed C–H amination reaction is described. The use of a chiral BINOL phosphoric acid ligand enables the conversion of readily available amines into synthetically valuable aziridines in high enantiomeric ratios. The aziridines can be derivatized to afford a range of chiral amine building blocks incorporating motifs readily encountered in pharmaceutically relevant molecules