Sumit K. Singh, Danish Ansari, Anindra Sharma, V. Tiwari
ABSTRACT The 1,3‐dipolar cycloaddition reaction of alkyne and azide, known as click chemistry, is one of the most effective and popular approaches for selective C─N bond forming reactions, resulting in the synthesis of 1,2,3‐triazoles. The 1,2,3‐triazole analogues have a wide range of importance, including medicinal, catalytic, and many more. These compounds are widely accessible through transition‐metal catalysts, such as copper‐ and ruthenium‐catalyzed azide‐alkyne cycloaddition reactions. In contrast, an environmentally benign organocatalyzed route is considered one of the best alternative approaches to assemble 1,2,3‐triazole analogues with good sustainability and has been well‐suited for application in biological systems. This tutorial review highlights the recent advances with growing scope and associated challenges ahead about the organocatalyzed click‐mediated development of the 1,2,3‐triazole‐linked biocompatible molecules, along with their mechanistic insights.