Cu(I)-catalyzed azide-alkyne 1,3-dipolar cycloaddition (Cue-AAC), which is the best paradigm of “Click Chemistry” philosophy that was initially coined by Sharpless and co-workers at the very beginning of the third millennium, has been demonstrated as a powerful tool in numerous scientific fields including medicinal chemistry, materials science, etc., due to its superior stereoselectivity, modularity and functional group tolerance. Meanwhile, microwave irradiation has attracted increasingly much attention as a highly effective and green synthetic complement as this technique can distinctly reduce the time consumption and simultaneously enhance the yields and purity of a diverse range of organic reactions in comparison with conventional heating methods. Herein, recent tactics that combine Cue-AAC with microwave irradiation technique toward the construction of useful bio-macromolecules and small molecule libraries are reviewed while the prospective with respect to the future development of this specific area is offered.

Key words: click chemistry, microwave-assisted, organic synthesis, bio-macromolecules, small molecules, green chemistry