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A series of novel gem-dimethyl-bearing SGLT2 inhibitors 1 were designed based on the structure of Dapagliflozin.They were synthesized through an efficient approach with anhydrous aluminum chloride-mediated Friedel-Crafts alkylation being the key step.Biological evaluations with in vivo models revealed that most of these compounds showed potent SGLT2 inhibitory activity and antihyperglycemic activity.