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Synthesis of two metabolites of edaravone

Xin-Rong Zhu, Yi Zheng, Peng Wang, Shi-Bao Yang, Rong Chen, Yong-Qiang Zhu*   

  1. Jiangsu Simcere Pharmaceutical Research Institute and Jiangsu Key Laboratory of Molecular Targeted Antitumor Drug Research, Nanjing 210042, China
  • Received:2010-01-12 Revised:2010-06-10 Online:2010-07-15 Published:2010-07-15
  • Contact: Yong-Qiang Zhu*

Abstract:

Edaravone glucuronate and edaravone sulfate, two metabolites of edaravone, were synthesized in improved yields. Edaravone glucuronate was synthesized by conjugation of edaravone with glucuronolactone through a series of reactions. Edaravone sulfate was synthesized through sulfonation of edaravone. Compared with the reported methods in the literature, the yields of both metabolites with the improved methods were much higher.

Key words: Edaravone, Glucuronate, Sulfate, Metabolite

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