Abstract

CuCl catalyzes efficient synthesis of aminoindolizine scaffolds by one-pot reactions in PEG of pyridine- or quinoline-2-carboxaldehydes with secondary amines and terminal alkynes via tandem C–H activation, coupling, and cyclization reactions. The reactions are easy to perform, atom-economic, environment friendly, broad in scope, and allow the generation of a number of biologically potent aminoindolizine frameworks from readily accessible starting materials.

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