Iridium‐Catalyzed Asymmetric Allylic Amination with Polar Amines: Access to Building Blocks with Lead‐Like Molecular Properties

Abstract

Abstract The combination of an air‐stable iridium catalyst and the dipolar aprotic solvent dimethyl sulfoxide (DMSO) allowed, for the first time, the systematic exploitation of highly polar, functionalized amines in asymmetric allylic substitutions: low molecular weight, sp 3 ‐rich chiral building blocks were obtained with physicochemical properties that will be valuable in the synthesis of lead‐like small molecules.