自由基清除剂依达拉奉（MCI - 186，必存）代谢产物的合成。

Synthesis of the metabolites of a free radical scavenger edaravone (MCI-186, Radicut).

作者信息

Watanabe Kazutoshi, Taniguchi Masao, Shinoda Masaki

机构信息

Research and Development Division, Mitsubishi Pharma Corporation, Yokohama, Japan.

出版信息

Redox Rep. 2003;8(3):157-61. doi: 10.1179/135100003225001539.

DOI:10.1179/135100003225001539

PMID:12935313

Abstract

Two metabolites of a free radical scavenger, edaravone, were synthesized. Edaravone glucuronate was synthesized by glycosylation of a glucuronic acid precursor using silver (I) trifluoromethane-sulfonate with edaravone. Edaravone sulfate was synthesized by sulfonylation of edaravone using a sulfur trioxide-pyridine complex. The two synthesized metabolites were identical to isolated metabolites. X-ray analysis identified edaravone glucuronate as beta-O-glucuronate, although there were three possible edaravone glucuronate tautomers.

摘要

合成了自由基清除剂依达拉奉的两种代谢产物。依达拉奉葡萄糖醛酸苷是通过使用三氟甲磺酸银使葡萄糖醛酸前体与依达拉奉进行糖基化反应合成的。依达拉奉硫酸盐是通过使用三氧化硫 - 吡啶络合物对依达拉奉进行磺酰化反应合成的。这两种合成的代谢产物与分离得到的代谢产物相同。X射线分析确定依达拉奉葡萄糖醛酸苷为β - O - 葡萄糖醛酸苷，尽管依达拉奉葡萄糖醛酸苷存在三种可能的互变异构体。