Asymmetric Aziridination of N-Sulphonyl Ketimines with Unfunctionalized Ketones: A One-pot Approach to Multisubstituted Fused Aziridines.

A highly diastereo- and enantioselective aziridination of N-sulphonyl ketimines with unfunctionalized ketones was reported. In this efficient method, a sequential direct asymmetric Mannich reaction and oxidative C-H amination were involved, which enabled a straightforward route to multisubstituted-fused aziridines in one pot. More importantly, two different products could be selectively obtained in the reaction by adding or removing a metal additive.