Copper-catalyzed 1,3-aminoazidation of arylcyclopropanes: a facile access to 1,3-diamine derivatives

Abstract

Copper-catalyzed 1,3-aminoazidation of arylcyclopropanes with N-fluorobenzenesulfonimide (NFSI) and trimethylsilyl azide (TMSN₃) has been established, facilely and efficiently affording a wide range of 1,3-diamine derivatives in moderate to good yields under mild conditions. It represents the first example of 1,3-diamination of cyclopropanes by simultaneously introducing two different nitrogen sources, which might provide a new route to ring-opening 1,3-bisfunctionalization of cyclopropanes.