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A simple copper catalyzed “one‐pot” process has been developed for synthesis of polysubstituted imidazoles viadirect oxidative N‐α‐C(sp3)‐Hfunctionalization of arylmethylamines. The readily available arylmethylamines as a substrate have afforded tetrasubstituted imidazoles products up to 94% yields under mild and environmentally benign conditions. The explored substrates scope with 1,2‐diketones and α‐hydroxyketones have shown great utility for synthesis of tetrasubstituted imidazoles. A simple copper‐catalyzed“one‐pot” process has been developed for synthesis of polysubstituted imidazoles viadirect oxidative N‐α‐C(sp3)‐Hfunctionalization of arylmethylamines. The readily available arylmethylamines as a substrate have afforded tetrasubstituted imidazoles products up to 94% yields under mild and environmentally benign conditions. The explored substrates scope with 1,2‐diketones and α‐hydroxyketones have shown great utility for synthesis of tetrasubstituted imidazoles.

A simple copper‐catalyzed“one‐pot” process has been developed for the synthesis of poly‐substituted imidazoles. Tetrasubstituted imidazoles could be afforded in short reaction time and in excellent yields under mild and eco‐friendly conditions viadirect oxidative N‐α‐C(sp3)‐Hfunctionalization of arylmethylamines. The explored substrate scope of readily available benzylamines with 1,2‐diketones and α‐hydroxyketones has shown great utility in designing different tetrasubstituted imidazole scaffolds that are of medicinal significance through this alternative route. More information can be found in the Research Article by Vikas D. Kadu et al.