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1,2-cis-Glycosides have both biological and chemical significance. Their presence in natural compounds influences taste, biological activity and drug development. Additionally, their syntheses provide avenues for chemical research and potential therapeutic applications. The construction of 1,2-cis-glycosidic bonds is still a major challenge in carbohydrate synthesis. Although most organic chemists crave general methods, glycosylation reactions continue to be a challenge. Since these reactions are highly dependent on the donor–acceptor pair, the solvent and reagents/catalysts/promoters, one should design the perfect donor and fine-tune the reaction conditions accordingly to obtain the desired stereochemical outcome. New methodologies and studies reveal solutions that may not be universal but can be the key to unsolved problems. In this chapter, recent methods for the synthesis of 1,2-cis-glycosides are highlighted.

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