• 中国精品科技期刊
  • 中国高校百佳科技期刊
  • 中国中文核心期刊
  • 中国科学引文数据库核心期刊
Advanced Search
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
shu

A new synthetic process of dapagliflozin

More Information
    Graphical Abstract
    • Abstract
  • 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.
    • FullText(HTML)
    • References (6)
  • [1]
    Tang Q,Li X,Song P,et al.Optimal cut-off values for the homeostasis model assessment of insulin resistance(HOMA-IR)and pre-diabetes screening:developments in research and prospects for the future[J].Drug Discov Ther,2015,9(6):380-384.
    [2]
    Mather A,Pollock C.Glucose handling by the kidney[J].Kidney Int Suppl,2011,79(2):S1-S6.
    [3]
    Meng W,Ellsworth BA,Nirschl AA,et al.Discovery of dapagliflozin:a potent,selective renal sodium-dependent glucose cotransporter 2(SGLT2)inhibitor for the treatment of type 2 diabetes[J].J Med Chem,2008, 51(5):1145-1149.
    [4]
    Xu BH,Lv BH,Xu G,et al.Process for preparation of benzylbenzene sodium-dependent glucose cotransporter 2(SGLT2)inhibitors:WO,2013152476[P].2013-10-17.
    [5]
    Lemaire S,Houpis IN,Xiao T,et al.Stereoselective C-glycosylation reactions with arylzinc reagents[J].Org Lett,2012, 14(6):1480-1483.
    [6]
    Zhang WW,Dai ZQ,Zhang ZY,et al.Progress in transition-metal-catalyzed cross-coupling reaction of grignard reagent with halides[J].Chem World(化学世界),2001,52(3):314-316.
    • Related Articles

Catalog

    Get Citation
    PDF
    XML
    Article views (1005) PDF downloads (2978) Cited by()
    Turn off MathJax
    Article Contents
    Abstract
    References

    Copyright © Journal of China Pharmaceutical University苏ICP备12050101号-2

    Address：24 Tongjia Lane, Nanjing City, Jiangsu Province （210009）Tel: 025-83271566E-mail: xuebao@cpu.edu.cn

    Supported by: Beijing Renhe Information Technology Co., Ltd.  Baidu Analytics

    Total visits：414976

    /

    DownLoad:  Full-Size Img  PowerPoint
    Return
    Return