New supported catalysts for the Huisgens [3 + 2] azide-alkyne cycloaddition have been prepared by immobilization of copper species on commercially available polymeric matrixes incorporating the 1,5,7-triazabicycloAThe synergic exploitation of the exceptional copper chelating ability and basicity profile of the TBD framework, in addition to ensuring effective immobilization and stabilization of copper species, allows the implementation of three-component strategies. The new catalytic systems enabled the development of regioselective, efficient, modular, mild and eco-friendly multicomponent syntheses of diversely decorated 1,2,3-triazoles, contributing to expand the scope and versatility of the Cu-catalyzed Huisgen 1,3-dipolar cycloaddition.

We herein document the first example of a reliable copper-catalyzed Huisgen 1,3-dipolar cycloaddition under oxidative conditions. The combined use of two polymer-supported reagents (polystyrene-1,5,7-triazabicyclo[4,4,0]dec-5-ene/Cu and polystyrene-2-iodoxybenzamide) overcomes the thermodynamic instability of copper(I) species toward oxidation, enabling the reliable Cu-catalyzed Huisgen 1,3-dipolar cycloadditions in the presence of an oxidant agent. This polymer-assisted pathway, not feasible under conventional homogeneous conditions, provides a direct assembly of 4-acyl-1-substituted-1,2,3-triazoles, contributing to expand the reliability and scope of Cu(I)-catalyzed alkyne-azide cycloaddition.

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