Sinclair Pharmaceuticals Limited

Llorenç Rafecas Jane

Nicolas Tesson

Alexander Christian Comely

Antoni Riera Escale

Atoni Escale Riera

It comprises a process for the production of delmopinol or a pharmaceutically acceptable salt and/or a solvate thereof, by subjecting the compound of formula (II) where R1 and R2 are the same or different, independently selected from the group consisting of H, (C1-C6) alkyl or, alternatively, R1 and R2 form, together with the carbon atom to which they are attached, a (C5-C6) cycloalkyl radical; and R3 is a radical selected from the group consisting of CF3, (C1-C4) alkyl, phenyl, and phenyl mono- or disubstituted by a radical selected from the group consisting of (C1-C4)-alkyl, halogen and nitro to a deprotection and cyclisation reaction. The process is useful to prepare delmopinol or its salts on an industrial scale. The compound of formula (II) is new and also forms part of the present invention, as well as its preparation process and other new intermediates of said preparation process. 

Preparation of delmopinol

It comprises a preparation process of delmopinol or a pharmaceutically acceptable salt and/or a solvate thereof, by submitting the compound of formula (II) where Rand Rare the same or different, independently selected from the group consisting of H, (C-C)-alkyl or, alternatively, Rand Rform, together with the carbon atom to which they are attached, a (C-C)-cycloalkyl radical; and Ris a radical selected from the group consisting of CF, (C-C)-alkyl, phenyl, and phenyl mono- or disubstituted by a radical selected from the group consisting of (C-C)-alkyl, halogen and nitro to a deprotection and cyclisation reaction. The process is useful to prepare delmopinol or its salts on an industrial scale. The compound of formula (II) is new and also forms part of the present invention, as well as its preparation process and other new intermediates of said preparation process. 

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Llorenç del Penedes, Spain

Llorenç Rafecas Jane