Process for the preparation of 2-[(diphenylmethyl) thio]...

C - Chemistry – Metallurgy – 07 – C

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C07C 319/20 (2006.01) C07C 315/02 (2006.01) C07C 317/28 (2006.01) C07C 323/29 (2006.01) C07C 323/56 (2006.01)

Patent

CA 2514900

Process for the preparation of 2-[(diphenylmethyl)thioacetamide, an intermediate for the preparation of Modafinil which is a CNS stimulant and used for the treatment of narcolepsia. The process comprises reacting 2- [(diphenylmethyl)thio]acetic acid with alcohols, in presence of catalytic amount of inorganic acid or organic acid at reflux temperature of alcohol to obtain corresponding ester which is reacted with ammonia to give 2- [(diphenylmethyl)thio]acetamide. If desired 2-[(diphenylmethyl)thioacetamide thus produced is reacted with hydrogen peroxide to produce Modafinil.

L'invention concerne un procédé de préparation de 2-[(diphénylméthyl)thioacétamide, qui est un intermédiaire pour la préparation de modafinil, lequel est un stimulant du système nerveux central et est utilisé pour le traitement de la narcolepsie. Le procédé selon l'invention consiste à faire réagir de l'acide 2-[(diphénylméthyl)thioacétique avec des alcools en présence d'un taux catalytique d'acide inorganique ou d'acide organique à une température de reflux de l'alcool afin d'obtenir l'ester correspondant qu'on fait réagir avec de l'ammoniaque afin d'obtenir le 2-[(diphénylméthyl)thioacétamide. Si on le souhaite, on peut faire réagir le 2-[(diphénylméthyl)thioacétamide ainsi obtenu avec du peroxyde d'hydrogène afin de produire le modafinil.

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