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

J Am Chem Soc. 2017 Feb 1;139(4):1412-1415. doi: 10.1021/jacs.6b12234. Epub 2017 Jan 18.

Abstract

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.

Publication types

  • Research Support, Non-U.S. Gov't