Process for manufacturing optically pure (r) or...

C - Chemistry – Metallurgy – 07 – C

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C07C 303/42 (2006.01) C07B 57/00 (2006.01) C07C 311/37 (2006.01)

Patent

CA 2560347

The invention relates to an improved process for the manufacture of enantiomerically pure R-(+) or S-(+)-5-(2-aminopropyl)-2-methoxybenzene sulfonamide by resolution of (R,S)-5-(2-aminopropyl)-2-methoxybenzene sulfonamide with D-(-) or L-(+)-tartaric acid to form a mixture of diastereomeric salts, separating the diastereomeric salts by kinetic resolution in a mixture of solvent systems of the kind such as herein described, in the specified time and temperature range to provide said R-(-)-5- (2-aminopropyl)-2-methoxybenzene sulfonamide or S-(+)-5-(2-aminopropyl)-2- methoxybenzenesulfonamide with excellent chiral purity more than 99.9 %.

L'invention concerne un procédé amélioré de production de R-(+) ou S-(+)-5-(2-aminopropyl)-2-méthoxybenzène sulfonamide énantiomériquement pur par résolution de (R, S)-5-(2-aminopropyl)-2-méthoxybenzène sulfonamide avec D-(-) ou L-(+)-acide tartarique pour former un mélange de sels diastéréomères, par une résolution cinétique dans un mélange de systèmes de solvants du type de ceux ici décrits, dans la gamme de temps et de températures spécifiée pour produire ledit R-(-)-5-(2-aminopropyl)-2-méthoxybenzène sulfonamide ou S-(+)-5-(2-aminopropyl)-2-méthoxybenzènesulfonamide avec une pureté chirale excellente de plus de 99,9 %.

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