Kinetic Resolution of 2H‐Azirines by Asymmetric Imine Amidation

Abstract Highly efficient kinetic resolution of 2 H ‐azirines by an asymmetric imine amidation was achieved in the presence of a chiral N , N ′‐dioxide/Sc III complex, thus providing a promising method to obtain the enantioenriched 2 H ‐azirine derivatives and protecting‐group free aziridines at the same time. It is rare to find an example of N1 of an oxindole participating in a reaction over C3. Moreover, chiral 2 H ‐azirines were stereospecifically transformed into an unprotected aziridine and α‐amino ketone.