Efficient Construction of Atropisomeric Arylamines through a Diastereoselective Buchwald‐Hartwig Amination

Abstract A practical and efficient strategy using a Pd‐catalyzed intramolecular Buchwald‐Hartwig amination was reported. A broad range of atropisomeric arylamines were obtained with excellent diastereoselectivities and yields. Even the N‐alkyl substrates were synthesized smoothly. The reaction scale‐up and further transformations of selected arylamines also demonstrated the synthetic utility of this protocol.