A facile access to 3-heterosubstituted (3-oxazolidinonyl/indolyl/phenoxy) imidazo[1,2-a]pyridines from readily available 2-aminopyridines and electron-rich (internally activated) alkynes like ynamides/ynamines/ynol ethers is achieved via Cu(OTf)2-mediated intermolecular diamination under aerobic conditions. The reaction is highly regioselective, owing to internal electron bias, and thus led to a single regioisomer with heterosubstitution at C3.
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