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Chemistry, traditionally being the science of synthesis and structural manipulations of molecules, has gradually undertaken the more challenging task of biology-oriented synthesis. The generation of molecules/molecular assemblies possessing welldefined biological functions remains an extremely challenging task; immediate refinements in conventional synthetic tactics are necessary. New and more efficient chemical reactions and methodologies, which may override the laborious protection/deprotection and purification steps in conventional total synthesis, could revolutionize the next-generation chemical and biological research. A set of chemical reactions, known as bioorthogonal reactions, that are orthogonal to most functional groups in biological systems has so far shown promising applications in biological research. Of these reactions, the Cu(I)-catalyzed version of the Huisen 1,3-dipolar cycloaddition reaction between azides and terminal alkynes for the construction of trizoles, referred to as a ¡°click chemistry reaction¡±, was defined by nobel laureate KB Sharpless and associates in 2001. Click chemistry has recently emerged to become one of the most powerful tools in drug discovery, chemical biology, and proteomic applications. In recent years, the design and synthesis of pharmacologically relevant heterocyclic molecules by combinatorial techniques have proven to be a promising strategy in the search for new pharmaceutical lead structures. Click chemistry is one of the powerful reactions for making carbon−heteroatom−carbon bonds in aqueous environment with a wide variety of chemical and biological applications in various fields.

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