Synthesis of the metabolites of a free radical scavenger edaravone (MCI-186, Radicut) |
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| Authors: | Watanabe Kazutoshi Taniguchi Masao Shinoda Masaki |
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| Affiliation: | Research and Development Division, Mitsubishi Pharma Corporation, Yokohama, Japan. Watanabe.Kazutoshi@mb.m-pharma.co.jp |
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| 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. |
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