Synthesis of two metabolites of edaravone

依达拉奉代谢产物的合成(英文)

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.

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-SO_3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。