C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 471/04 (2006.01)
Patent
CA 2344439
The present invention relates to an improved process for the production of the methanesulfonate sesquihydrate which comprises direct salt and hydrate formation. According to the invention there is provided a process for the production of 7-(3-aminomethyl -4-syn -methoxyiminopyrrolidin -1-yl)-1 -cyclopropyl -6-fluoro -4-oxo- 1, 4-dihydro - 1, 8-naphthyridine -3-carboxylic acid methanesulfonate sesquihydrate which comprises reacting 7-(3-aminomethyl -4-syn - methoxyiminopyrrolidin -1-yl)-1 -cyclopropyl -6-fluoro -4-oxo-1, 4-dihydro -1, 8-naphthyridine -3-carboxylic acid of formula (I) having antibacterial activity and methanesulfonic acid in a solvent comprising at least onw water miscible cosolvent and water, and isolating the resulting solid product.
L'invention concerne un procédé amélioré destiné à la fabrication de sesquihydrate de méthanesulfonate qui consiste à former directement le sel et l'hydrate. L'invention se rapporte à un procédé destiné à la fabrication de sesquihydrate de méthanesulfonate de l'acide 7-(3-aminométhyl-4-syn-méthoxy-iminopyrrolidin-1-yl)-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxylique qui consiste à faire réagir l'acide 7-(3-aminométhyl-4-syn-méthoxy-iminopyrrolidin-1-yl)-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxylique correspondant à la formule (I) et possédant une activité antibactérienne et l'acide méthanesulfonique dans un solvant comprenant au moins un co-solvant miscible à l'eau et de l'eau puis à isoler le produit solide qui en résulte.
Hayes Jerome Francis
Walsgrove Timothy Charles
Wells Andrew Stephen
Borden Ladner Gervais Llp
Lg Life Sciences Limited
Smithkline Beecham P.l.c.
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