Advances on the Synthesis of C-Aryl-glycosides Since 2019

Abstract Aryl-glycosides represent a significant subclass of crucial glycosidic compounds, increasingly capturing the attention of pharmaceutical developers as bioelectronic motifs embedded within glycosides. Their outstanding resistance to enzymatic hydrolysis bestows a distinctive advantage in the field of drug development, particularly in therapeutic domains such as diabetes treatment, where pharmaceuticals based on the C-aryl-glycoside architecture manifest compelling therapeutic efficacy. As a result, researchers in the realm of synthetic chemistry have diligently explored and devised a plethora of streamlined and efficacious synthetic methodologies. This comprehensive account systematically delineates methodologies employed in recent years for the efficient synthesis of C-aryl-glycosides, offering insights into three primary directions: transition-metal catalysis, radical strategies, and metal-free catalysis processes. 1 Introduction 2 Glycosylation via Transition-Metal Catalytic Approaches 3 Glycosylation via Glycosyl Radical Approaches 4 Glycosylation via Metal-Free Catalytic Approaches 5 Conclusion and Outlook