Stereoselective synthesis of trans-aziridines via intramolecular oxidative C(sp3)–H amination of β-amino ketones

Abstract

Aziridines are ubiquitous in bioactive molecules and often serve as key synthetic building blocks. We report herein an intramolecular KI/TBHP mediated oxidative dehydrogenative C(sp³)–H amination reaction to synthesize a diverse array of trans-2,3-disubstituted aziridines in good yields under mild conditions. The synthetic utility of this protocol was further highlighted by a one-pot, two-step synthesis of unprotected aziridines.