Environmentally Benign Click Chemistry: A Path to Biologically Active Triazoles

Abstract Click chemistry has revolutionized synthetic methodologies by offering efficient, selective, and environmentally benign approaches to molecular assembly. Among these, the copper(I)‐catalyzed azide‐alkyne cycloaddition (CuAAC) has emerged as a key strategy for the green synthesis of triazole‐based molecules, renowned for their stability, biocompatibility, and broad‐spectrum biological activities. The environmentally friendly nature of click chemistry, characterized by atom economy, reduced waste, and the use of benign solvents aligns with the growing emphasis on sustainable drug discovery. This review explores recent advancements in the green synthesis of biologically active triazoles via click chemistry, with a focus on their applications in antimicrobial and anticancer research. Additionally, alternative click approaches such as strain‐promoted azide‐alkyne cycloaddition (SPAAC) is discussed in the context of biorthogonal applications, highlighting their impact on chemical biology. By integrating these sustainable strategies, the development of functionalized triazoles presents a promising avenue for biomedical innovation while addressing the urgent need for eco‐conscious synthetic practices.