Palladium-catalyzed enantioselective C-H activation of aliphatic amines using chiral anionic BINOL-phosphoric acid ligands

© 2017 American Chemical Society. 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