Cu(I)-catalyzed azide-alkyne 1,3-dipolar cycloaddition (CuAAC), popularly known as the "click reaction", serves as the most potent and highly dependable tool for facile construction of simple to complex architectures at the molecular level. Click-knitted threads of two exclusively different molecular entities have created some really interesting structures for more than 15 years with a broad spectrum of applicability, including in the fascinating fields of synthetic chemistry, medicinal science, biochemistry, pharmacology, material science, and catalysis. The unique properties of the carbohydrate moiety and the advantages of highly chemo- and regioselective click chemistry, such as mild reaction conditions, efficient performance with a wide range of solvents, and compatibility with different functionalities, together produce miraculous neoglycoconjugates and neoglycopolymers with various synthetic, biological, and pharmaceutical applications. In this review we highlight the successful advancement of Cu(I)-catalyzed click chemistry in glycoscience and its applications as well as future scope in different streams of applied sciences.

Tris(pentafluorophenyl)borane-promoted stereoselective glycosylation with trichloroacetimidate glycosyl donors is described. The reactions proceed efficiently with a wide range of acceptors, from sugar to nonsugar, under mild conditions in the presence of a catalytic amount of B(CF). The perbenzylated glucosyl α-imidate provides β-selective glycosides in 70-92% yields.

The synthesis of triazolyl azido alcohols from terminal alkyne via oxirane ring-opening of epichlorohydrin, followed by click reaction with alkynes, and subsequent azidation of chlorohydroxy triazoles was achieved under a one-pot methodology. The developed triazolyl azido alcohols were further utilized for the synthesis of a diverse range of morpholine-fused triazoles of chemotherapeutic value. The structure of all developed compounds has been elucidated using IR, NMR, MS, and elemental analysis, where four of them have been characterized by single-crystal X-ray analysis.

A number of novel 7-O-noscapine glycoconjugates have been synthesized starting from Noscapine, an alkaloid found in opium plant, via two successive steps. First step is the selective 7-O-demethylation of Noscapine and the next one is the subsequent propargylation which afford 7-O-propargyl noscapine (3) in good yield. The structure of was confirmed by extensive spectroscopic data including single crystal X-ray. The 1,3-dipolar cycloaddition of developed noscapine derivative 3 with glycosyl azides 6a-m was investigated to give the triazole linked second-generation noscapine analogous in their glycoconjugate forms (8a-m) to augment the therapeutic efficacy of noscapine.

Newly synthesized Cu(i) with thiobenzoate complexes was found to catalyse the regioselective synthesis of glycoconjugate triazoles under click reaction.