Abstract Three novel gem-dimethyl C-glucosides were designed as sodium-glucose co- transporter 2 (SGLT2) inhibitors, and their syntheses started from D-glucose and three 2- substituted-5-bromobenzoic acids were achieved via a facile 8-step protocol, with the key step being anhydrous aluminum chloride-catalyzed Friedel-Crafts alkylation of tertiary alcohols and phenetol. These three SGLT2 inhibitors were evaluated in vivo with a mice ...