Preparation of levofloxacin and forms thereof

Details Preparation of levofloxacin and forms thereof Preparation of levofloxacin and forms thereof

C - Chemistry, Metallurgy

07

D

C07D 498/06 (2006.01)

Patent

CA 2462023

Levofloxacin was prepared by reacting (S)-(-)-9,10-difluoro-3-methyl-7-oxo-2,3- dihydro-7H-pyrido[1,2,3-de][1,4]benzoxazine-6-carboxylic acid with N-methyl piperazine in a polar solvent or in a neat mixture to form levofloxacin. Further processing of the levofloxacin produced novel levofloxacin forms, including a hemihydrate and Forms A, B, C, F, G and H.

On produit, dans le cadre de ce procédé de la lévofloxacine en faisant réagir de l'acide carboxylique (S)-(-)-9,10-difluoro-3-méthyl-7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzoxazine-6 avec de la N-méthyl pipérazine dans un solvant polaire ou dans un mélange absolu. Un traitement ultérieur de cette lévofloxacine permet de produire de nouvelles formulation de lévofloxacine, notamment un semi-hydrate ainsi que les formes A, B, C, F, G et H.

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