N-demethylation of cyamemazine via non-classical Polonovski reaction and its conjugation to bovine serum albumin

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• 作者：Gurmit Singh^a ; ^{gurmit.singh@hc-sc.gc.ca} ; Terry B. Koerner^a ; Samuel Benrejeb Godefroy^b ; Claude Armand^c
• 关键词：Cyamemazine ; Monodesmethyl cyamemazine ; Hapten and Polonovski reaction
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2012
• 期刊代码：10_0960894x
• 类别：ch
• 出版时间：15 March, 2012
• 卷：22
• 期：6
• 页码：2160-2162
• 文件大小：214 K

摘要

A modified Polonovski reaction has been employed to obtain the N-demethylated metabolite of the neuroleptic drug cyamemazine. The synthesis involves N-oxide formation, isolation of the corresponding N-oxide, and a FeSO₄路7H₂O mediated Polonovski reaction to afford the desired monodesmethyl cyamemazine. In a subsequent step the hapten N-demethylcyamemazine-hemiglutarate was synthesized and its conjugated to bovine serum albumin (BSA).