Copper-mediated C(sp3)–H amination in a multiple C–N bond-forming strategy for the synthesis of N-heterocycles

Abstract

An efficient construction of imidazo[1,5-a]pyridines, through a three-component reaction involving benzyl substituted pyridines, aldehydes, and TMSN₃, has been developed. Three C–N bonds were formed in one pot. Copper-promoted amination of the benzylic C(sp³)–H bond is a key step of this multiple C–N bond-forming sequence.