Abstract A novel synthetic approach for the preparation of bexagliflozin (1) , a selective inhibitor of sodium‐dependent glucose cotransporter 2 (SGLT‐2) utilized in the management of type 2 diabetes. This new method is designed to be simple and environmentally friendly, employing innovative intermediates and offering high efficiency in the production of compound (1) . The paper details the experimental procedures undertaken to assess this advanced and scalable synthetic route. Key features of the process include the use of commercially available and easily manageable reagents, reduced reaction steps, and minimized waste generation. This approach not only enhances the efficiency of the synthesis but also aligns with sustainable chemical practices.