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      Permanent link:
      https://www.ias.ac.in/article/fulltext/jcsc/132/0042

    • Keywords

       

      Dapagliflozin; SGLT2 inhibitor; Anti diabetic drug; Metabolites; Synthesis.

    • Abstract

       

      Dapagliflozin is one of the gliflozin class drugs, useful for the treatment of type-2 diabetes. Dapagliflozin undergoes extensive metabolism and transforms to metabolites in humans. The contribution of pharmacologically active metabolites in drug discovery and development is significant. A streamlined synthetic approach is devised to access three metabolites of dapagliflozin namely, benzylic hydroxy dapagliflozin, oxo dapagliflozin and desethyl dapagliflozin.Two synthetic protocols have been proposed for the synthesis of benzylic hydroxy dapagliflozin and oxo dapagliflozin. An enantioselective deethylation of dapagliflozin is also reported

    • Author Affiliations

       

      KISHORE KARUMANCHI1 2 SENTHIL KUMAR NATARAJAN1 RAMADAS CHAVAKULA1 RAGHU BABU KORUPOLU2 KISHORE BABU BONIGE2 BADARINADH GUPTA PERURI3

      1. Chemical Research and Development, APL Research Centre-II, Aurobindo Pharma Ltd., Survey No. 71 & 72, Indrakaran Village, Kandi Mandal, Sangareddy District, Telangana State 502329, India
      2. Department of Engineering Chemistry, A. U. College of Engineering (A), Andhra University, Visakhapatnam, Andhra Pradesh 530003, India
      3. Analytical Research and Development, APL Research Centre-II, Aurobindo Pharma Ltd, Survey No. 71 & 72, Indrakaran Village, Kandi Mandal, Sangareddy District, Telangana State 502329, India

    • Dates

       
      Published
      13 February 2020
      Manuscript received
      7 July 2019
      Manuscript revised
      21 December 2019
      Accepted
      5 January 2020

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