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

…, TB Koerner, SB Godefroy, C Armand

Index: Singh, Gurmit; Koerner, Terry B.; Godefroy, Samuel Benrejeb; Armand, Claude Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 6 p. 2160 - 2162

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Citation Number: 8

Abstract

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· 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 ...