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Synthetic Strategies toward SGLT2 Inhibitors
Organic Process Research & Development ( IF 3.4 ) Pub Date : 2018-03-30 00:00:00 , DOI: 10.1021/acs.oprd.8b00017
Anderson R. Aguillón 1 , Alessandra Mascarello 2 , Natanael D. Segretti 2 , Hatylas F. Z de Azevedo 2 , Cristiano R. W. Guimaraes 2 , Leandro S. M. Miranda 1 , Rodrigo O. M. A. de Souza 1
Affiliation  

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.

中文翻译:

SGLT2抑制剂的合成策略

格列净是一类重要的处方药,用于治疗II型糖尿病。它们通过靶向钠葡萄糖转运蛋白2(SGLT2)来降低血糖水平,因此抑制了肾脏中葡萄糖的重吸收。目前,有几种FDA批准的格列净,以及其他即将在未来几年内推出的药物。这篇综述描述了用于生产规模和工业规模的SGLT2抑制剂的合成策略。此外,突出了该策略的缺点以及多年来获得选择的格列净及其葡萄糖衍生物的改进。
更新日期:2018-03-30
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