Organocatalytic Atroposelective C−H Amination of Arenes with Indolines

Abstract An atroposelective synthesis of axially chiral N‐arylindolines has been established by organocatalytic nucleophilic amination of arenes with 7‐substituted indolines, providing a straightforward way to achieve the expected C−N atropisomers in good yields (up to 95 %) with good to excellent enantioselectivities (up to 97 % ee) from readily available starting materials. Furthermore, axially chiral N‐arylindole derivatives could be prepared upon oxidative aromatization of the corresponding N‐arylindolines.