Process of enantiomeric resolution of...

C - Chemistry – Metallurgy – 07 – D

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C07D 211/34 (2006.01)

Patent

CA 2674451

A process for preparing the d-threo isomer of methylphenidate hydrochloride which includes (i) resolving a racemic mixture of racemic threo-methylphenidate hydrochloride with a less than stoichiometric amount of tertiary amine base to obtain a methylphenidate - chiral acid salt, (ii) basifying the methylphenidate - chiral acid salt to obtain methylphenidate free base, and (iii) converting the methylphenidate free base into d-threo-methylphenidate hydrochloride

L'invention concerne un procédé de préparation de l'isomère d-thréo de l'hydrochlorure de méthylphénidate. Le procédé comprend les étapes consistant à : (i) séparer un mélange racémique d'hydrochlorure de thréo-méthylphénidate racémique avec une quantité inférieure à la quantité stoechiométrique d'une base amine tertiaire pour obtenir un sel acide chiral de méthylphénidate, (ii) basifier le sel acide chiral de méthylphénidate pour obtenir une base libre de méthylphénidate et (iii) transformer la base libre de méthylphénidate en hydrochlorure de d-thréo-méthylphénidate.

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