Method for the preparation of 5-cyanophthalide

C - Chemistry – Metallurgy – 07 – D

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C07D 307/88 (2006.01) C07D 307/87 (2006.01)

Patent

CA 2361395

A method for the preparation of 5-cyanophthalide in which 5-carboxyphthalide is reacted with a dehydrating agent, such as thionylchloride, and a sulphonamide, in particular sulfamide. Cyanophthalide is prepared in high yields by a convenient procedure. 5-Cyanophthalide is an intermediate used in the preparation of the antidepressant drug citalopram.

L'invention se rapporte à un procédé de préparation de 5-cyanophtalide selon lequel on fait réagir du 5-carboxyphtalide avec un agent déshydratant, tel que du chlorure de thionyle, et un sulfonamide, notamment un sulfamide. On prépare le cyanophtalide avec un très bon rendement en appliquant une procédure pratique. Le 5-cyanophtalide est un intermédiaire utilisé pour la préparation du médicament antidépresseur, le citalopram.

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