An improved process for the manufacture of montelukast sodium

Details An improved process for the manufacture of montelukast sodium An improved process for the manufacture of montelukast sodium

C - Chemistry, Metallurgy

07

D

C07D 215/18 (2006.01)

Patent

CA 2649189

Process for the manufacture of 1-[[[(1R)-1-[3-[(1E)-2-(7-chloro-2-quinolinyl)ethenyl]phenyl]-3-[2-(1-hydroxy-1-methylethyl)phenyl]propyl]thio]methyl]cyclopropane acetic acid, sodium salt [montelukast sodium (I)] consisting of: i. Converting methyl 1-(mercaptomethyl)-cyclopropaneacetate to a metal salt (X) using a metal hydroxide, ii. Subjecting the metal salt (X) to monometallation to provide a dimetallide (XI). iii. Converting a diol of formula (II) to a mesylate of formula (III) and reacting (III) in situ with (XI) affordin the metal salt of 1-[[[(1R)-1-[3-[(1E)-2-(7-chloro-2-quinolinyl)ethenyl]phenyl]-3-[2-(1-hydroxy-1-methylethyl)phenyl]propyl]thio]methyl]cyclopropane acetic acid. iv. Reacting the metal salt in-situ with a base and purifying to afford an amine salt (XII). v. Treating (XII) with a sodium base and precipitating out montelukast sodium (I).

Procédé pour la fabrication du sel de sodium de l'acide 1-[[[(1R)-1-[3-[(1E)-2-(7-chloro-2-quinoléinyl)éthényl]phényl]-3-[2-(1-hydroxy-1-méthyléthyl)phényl]propyl]thio]méthyl]cyclopropaneacétique [montélukast sodique (I)] consistant à : i) convertir du 1-(mercaptométhyl)-cyclopropaneacétate de méthyle en un sel de métal (X) en utilisant un hydroxyde de métal ; ii) soumettre le sel de métal (X) à une monométallation pour produire un dimétalide (XI) ; iii) convertir un diol de formule (II) en un mésylate de formule (III) et faire réagir (III) in situ avec (XI) pour produire le sel de métal de l'acide 1-[[[(1R)-1-[3-[(1E)-2-(7-chloro-2-quinoléinyl)éthényl]phényl]-3-[2-(1-hydroxy-1-méthyléthyl)phényl]propyl]thio]méthyl]cyclopropaneacétique ; iv) faire réagir le sel de métal in situ avec une base et purifier pour obtenir un sel d'amine (XII) ; v) traiter (XII) avec une base sodique et faire précipiter le montélukast sodique (I).

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