A process for the manufacture of zonisamide

Details A process for the manufacture of zonisamide A process for the manufacture of zonisamide

C - Chemistry, Metallurgy

07

D

C07D 261/20 (2006.01)

Patent

CA 2545119

The present invention describes an improved process for the preparation of 1,2Benzisoxazole-3-methanesulphonamide (Zonisamide), a well known anti- epileptic agent which possesses anti-convulsant and anti-neurotoxic effects. Other aspect of this invention are isolation of a key intermediate, viz., crystalline sodium chloride associated 1,2Benzisoxazole-3-methane sodium sulfonate (BOS-Na:NaCl). The isolated crude BOSNa:NaCl is directly converted to Zonisamide using controlled molar ratio of chlorosulfonic acid to avoid the disulfonated side products. The analytical characteristics like IR and XRD data of the BOS-Na:NaCl are also reported to confirm its nature.

La présente invention se rapporte à un procédé perfectionné de préparation de 1,2-benzisoxazole-3-méthanesulfonamide (Zonisamide), un agent anti-épileptique bien connu présentant des effets anti-convulsivants et anti-neurotoxiques. La présente invention se rapporte également à l'isolement d'un intermédiaire essentiel, à savoir le 1,2-benzisoxazole-3-méthane sodium sulfonate associé à du chlorure de sodium cristallin (BOS-Na:NaCl). Le BOS-Na:NaCl brut isolé est transformé directement en Zonisamide à l'aide d'un rapport molaire contrôlé d'acide chlorosulfurique afin éviter tout produit secondaire bisulfoné. Les caractéristiques analytiques, par exemple les données IR et XRD, du BOS-Na:NaCl sont également signalés dans le but de confirmer sa nature.

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