Copper-mediated intramolecular C(sp3)–H amination of alicyclic amines: regio- and site-selective access to imidazolidin-4-one

Abstract

An efficient copper-mediated intramolecular C(sp³)–H amination of alicyclic amine is developed. This amination protocol is performed under mild reaction conditions by using di-t-butyl peroxide (DTBP) as the oxidant, exhibiting a wide range of functional group tolerance and affording regio-selective products in up to 89% yield. Preliminary mechanistic studies indicated that a Cu(I)/Cu(III) reaction model is most likely to be involved in this C–H amination reaction.