Construction of N-Alkyl- and N-Arylaziridines from Unprotected Amines via C–H Oxidative Amination Strategy

A copper-promoted intramolecular C–H oxidative amination reaction between secondary amine (N–H) and C(sp3)–H at the benzylic position of azaarenes or α-position of ketones for the synthesis of aziridine derivatives has been developed. Moreover, a practical annulation of electron-deficient vinylarenes with an unprotected primary alkyl amine by a Yb(OTf)3–CuI relay system has also been reported. The reactions were carried out with oxygen as the sole oxidant to give the N-alkyl- and N-arylaziridines in good yields.