Process for the preparation of delmopinol and derivatives thereof

US8143463B2 · kind B2 · utility

Assignee

• SINCLAIR PHARMACEUTICALS LTD · GB

Inventors

• Juan Jose Artus Surroca · Vilanova i la Geltrú, ES
• David Fernandez Bleda · Castelldefels, ES
• Tommaso Iacoangeli · Roma, IT
• Jordi Lluis Tous · Tarragona, ES

Key dates

• Filing date: Dec 20, 2010
• Grant date: Mar 27, 2012
• Expiry date: Dec 20, 2030

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07F3/02
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

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 a 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.