Asymmetric [3+3] Cycloaddition of Donor−Acceptor Aziridines with N,N‐Dialkyl‐3‐vinylanilines to Construct Highly Functionalized Enantioenriched Tetrahydroisoquinolines

Abstract A diastereo‐ and enantioselective [3+3] cycloaddition of donor−acceptor aziridines with N , N ‐dialkyl‐3‐vinylanilines has been established using a Mg(OTf) 2 /bisoxazoline catalyst, providing highly functionalized tetrahydroisoquinolines in good yields and with high levels of stereocontrol. A wide variety of N , N ‐dialkyl‐3‐vinylanilines, such as m ‐ N , N ‐dimethylaminophenyl α,β‐unsaturated phenyl ketones and 3‐( m‐N , N ‐dimethylaminophenyl)acrylates, as well as donor−acceptor N ‐tosylaziridines, have been applied in this asymmetric catalytic protocol.