CuAAC ‘Click Chemistry’-Mediated Synthesis of 1,4-Disubstituted 1,2,3-Triazoles

The Cu(I)-catalyzed azide-alkyne cycloaddition (CuAAC), a model click chemistry reaction pivotal in synthesizing diverse 1,4-disubstituted 1,2,3-triazoles with great ease. This modular tool stands out due to its exceptional efficiency, regioselectivity, and mild reaction conditions and is thus considered one of the most versatile organic reactions investigated so far. The versatility of CuAAC is well demonstrated through its application in diverse fields such as catalysis, sensing, glycoscience, medicinal chemistry, material sciences, agriculture, bioconjugation, and polymer science. More effective and selective Cu-catalysts can further increase the use of CuAAC tool, and thus, this chapter briefly highlights the optimization of CuAAC parameters, its robustness, and adaptability in solidifying its status as a cornerstone in modern synthetic chemistry. The mechanistic pathway facilitated by copper catalysts providing insights into their role in enhancing reaction kinetics and specificity is also presented.