The direct C3-functionalization of quinoxalin-2(1H)-ones via C-H bond activation has recently attracted considerable attention, due to their diverse biological activities and chemical properties. This review will focus on the recent achievements, mainly including arylation, alkylation, acylation, alkoxycarbonylation, amination, amidation and phosphonation of quinoxalin-2(1H)-ones. Their mechanisms are also discussed.