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(sp2)-H and C(sp3)-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(sp2)-H or C(sp3)-H arylation of sugars bearing the directing group.