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

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journal contribution
posted on 17.02.2017, 00:00 by Sheng Zhang, Lijun Li, Lilan Xin, Wenmin Liu, Kun Xu
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.