Over the past decades, the evolution of molecular biology protocols and microscopy techniques has made it possible to visually detect proteins in living systems with valuable spatiotemporal resolution, in which dynamic topological information has proved to be insightful. Natural products and synthetic small molecules can be used to perturb, dissect and manipulate biological processes, thereby providing the basis for drug development. Hopefully, in the next decade, we will witness the emergence of 1,2,3-triazole-bearing drugs on the market as this click reaction is used more and more widely in the drug discovery.
However, the 1,2,3-triazole ring itself is not a commonly used pharmacophore and has rarely been found in marketed drugs, demonstrating that there are still some limitations during the use of 1,2,3-triazole in the molecules of drug candidates. This review provides an overview of a most important click reaction, 1,3-dipolar cycloadditions of alkynes and azides, in the drug discovery.Ĭlick chemistry is a very powerful tool, in the drug discovery, because it is very efficient in the creation of compound libraries through combinatorial methodology. Furthermore, this reaction has been used increasingly in drug discovery, because the formed 1,2,3-triazole can act as both a bioisostere and a linker. This reaction is also near-perfect, in terms of its robustness, due to the high degree of reliability and complete specificity. The copper(I)-catalyzed 1,3-dipolar cycloaddition of alkynes and azides to form 1,2,3-triazoles is the most popular reaction in click chemistry. Such types of reported reactions and their reaction pathways are presented here in this minireview, which manifested the oxidative abilities and advantageous features of dialkyl azodicarboxylates. Very recently, these azo compounds have also been explored in photochemical reactions. Moreover, they have been utilized in different types of bond construction like C-Heteroatom (C-Het) and S−N bond. These azo compounds have been utilized as an oxidant or dehydrogenating reagent in oxidative transformations, such as cross dehydrogenative coupling, oxidative Ugi-type reaction, dehydrogenation etc. In recent past, dialkyl azodicarboxylates have been embraced as versatile reagents in synthetic strategies other than Mitsunobu reactions. Moreover, synthetic procedures and reaction pathways of these selected reactions are also highlighted. A brief summary of recent organic transformations mediated by dialkyl azodicarboxylates, popularly known for Mitsunobu reaction, is given in this minireview.
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