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

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

Bioorganic & medicinal chemistry letters (2012-03-01)
Gurmit Singh, Terry B Koerner, Samuel Benrejeb Godefroy, Claude Armand
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 FeSO(4)·7H(2)O 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).

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Sigma-Aldrich
Cyamemazine, ≥98% (HPLC)