Process for the preparation of delmopinol and derivatives...

C - Chemistry – Metallurgy – 07 – D

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C07D 265/30 (2006.01) C07D 295/08 (2006.01) C07D 498/04 (2006.01) C07F 3/02 (2006.01)

Patent

CA 2628921

A process for the preparation of delmopinol (3-(4-propylheptyl)-4- morpholinethanol) or a derivative or a pharmaceutically acceptable salt, or a solvate thereof, including an hydrate, comprises reacting oxazolidin [2, 3-c] morpholine and a grignard reagent, and optionally converting the delmopinol (or derivative) free base into a pharmaceutically acceptable salt. The oxazolidin [2, 3-c] morpholine and the grignard reagent are useful as intermediates in the production process.

La présente invention concerne un procédé pour la préparation de delmopinol (3-(4-propylheptyl)-4-morpholinéthanol) ou d~un dérivé ou un sel pharmaceutiquement acceptable, ou d~un solvate de celui-ci, notamment un hydrate, qui consiste à faire réagir de l~oxazolidin [2, 3-c] morpholine avec un réactif de Grignard, et éventuellement à convertir la base libre de delmopinol (ou son dérivé) en un sel pharmaceutiquement acceptable. L~oxazolidin [2, 3-c] morpholine et le réactif de Grignard sont utiles en tant qu~intermédiaires dans le procédé de production.

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