依达拉奉代谢产物的合成

依达拉奉代谢产物的合成

朱新荣, 郑毅, 王鹏, 杨士豹, 陈荣, 朱永强^*

江苏先声药物研究院江苏省抗肿瘤分子靶向药物研究重点实验室, 江苏南京 210042

收稿日期:2010-01-12 修回日期:2010-06-10 出版日期:2010-07-15 发布日期:2010-07-15
通讯作者: 朱永强*

Synthesis of two metabolites of edaravone

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

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*

摘要/Abstract

摘要：

本文设计了一种简便、高收率合成依达拉奉葡萄糖醛酸化和硫酸化两个代谢产物的方法。依达拉奉葡萄糖醛酸以葡萄糖醛酸内酯为原料, 经过一系列反应, 最终与依达拉奉成苷键来制备; 依达拉奉硫酸化产物通过依达拉奉与吡啶-SO3络合物发生硫酸化反应制备。和文献方法相比, 改进后的方法合成两个代谢产物的产率大大提高。

关键词: 依达拉奉, 葡萄糖醛酸化, 硫酸化, 代谢产物

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

中图分类号:

R916.42

Supporting:

Foundation item: Jiangsu Key Laboratory of Molecular Targeted Antitumor Drug Research Foundation (Grant No. BM2008201).
^*Corresponding author. Tel.: 86-25-85566666-1726; fax: 86-25-85566666-1835

朱新荣, 郑毅, 王鹏, 杨士豹, 陈荣, 朱永强^*

依达拉奉代谢产物的合成

[J]. .

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

Synthesis of two metabolites of edaravone

[J]. .

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