Process for the preparation of quaternary n-alkyl morphinan...

C - Chemistry – Metallurgy – 07 – D

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C07D 489/02 (2006.01)

Patent

CA 2504262

A process for the preparation of a quaternary derivative of the morphinan alkaloid, the process comprising contacting a tertiary N-substituted morphinan alkaloid with an alkyl halide in an anhydrous solvent system, wherein the solvent system comprises an aprotic dipolar solvent with the aprotic dipolar solvent constituting at least 25 wt % of the solvent system. Exemplary compounds include: (see formula 1) (see formula 1A).

L'invention concerne une méthode de préparation d'un dérivé quaternaire de l'alcaloïde morphinique. La méthode consiste à placer un alcaloïde morphinique tertiaire N-substitué au contact d'un halogénure d'alkyle, dans un système de solvants anhydres dont au moins les 25 % en poids sont constitués d'un solvant bipolaire aprotique.

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