Synthetic Strategies toward SGLT2 Inhibitors

AndersonR. Aguillón, Alessandra Mascarello, Natanael D. Segretti, Hatylas F. Z de Azevedo, Cristiano R. W. Guimaraes, Leandro S. M. Miranda, Rodrigo O. M. A. de Souza

Index: 10.1021/acs.oprd.8b00017

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Abstract

Gliflozins are an important class of prescription drugs used to treat type II diabetes. They reduce blood sugar levels by targeting the sodium-glucose transport protein 2 (SGLT2) and consequently inhibit glucose reabsorption in the kidney. There are currently several FDA-approved gliflozins as well as others in the pipeline to be launched in the next few years. This review describes the synthetic strategies used for manufacturing SGLT2 inhibitors on both bench and industrial scales. Moreover, the drawbacks to the strategies and the improvements made to obtain selected gliflozins and their glucose derivatives over the years are highlighted.