C–H Activation for the Synthesis of C1‐(hetero)aryl Glycosides

Because of the persistent need of drug discovery programs for simple methods to access bioactive C-aryl glycosides, the C–H activation approach has emerged as an efficient and sustainable alternative for classical reactions that limits the number of steps in a synthetic route as much as possible. In the present chapter, we highlight the different established strategies for C( sp 2 ) –H and C( sp 3 ) –H functionalization to access C -aryl glycosides. Two main strategies will be discussed: (a) C–H functionalization of aglycon partners bearing a directing group with different sugars as coupling partners (1-halosugras or glycals); and (b) C( sp 2 ) –H or C( sp 3 ) –H arylation of sugars bearing the directing group.