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MA Li, ZHANG Menghan, XU Zhiwei, SUN Ying′ai, ZHU Jing, HUANG Yingbo, ZHANG Dayong. A new synthetic process of dapagliflozin[J]. Journal of China Pharmaceutical University, 2017, 48(1): 42-45. DOI: 10.11665/j.issn.1000-5048.20170106
Citation: MA Li, ZHANG Menghan, XU Zhiwei, SUN Ying′ai, ZHU Jing, HUANG Yingbo, ZHANG Dayong. A new synthetic process of dapagliflozin[J]. Journal of China Pharmaceutical University, 2017, 48(1): 42-45. DOI: 10.11665/j.issn.1000-5048.20170106
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A new synthetic process of dapagliflozin

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  • This paper describes a practical process for a SGLT2 inhibitor dapagliflozin. The target product was synthesized from 1-chloro-2-(4-ethoxybenzyl)-4-iodobenzene and 2, 3, 4, 6-tetra-O-acetyl-alpha-D-glucopyranosyl bromide by iodine-magnesium exchange, and coupling and acetyl removing reactions with the total yield of 50%. This practical process highlights fewer reaction steps, less waste and mild reaction conditions.
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