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US 2006/0040874 A1Published application
Process for the preparation of topiramate
AssigneesHelm AG, CF Pharma Gyogyszergyarto KFT
InventorsGeza Arvai, Sandor Garaczi, Attila Mate, Ferenc Lukacs, Zsolt Viski, Geza Schneider
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Abstract
The present invention relates to a process for the preparation of topiramate, intermediates in this process and a process for the preparation of these intermediates.
Claims20
A process for the preparation of topiramate or a pharmaceutically acceptable salt thereof, which process comprises the step of hydrolysing a compound of the general formula IX:
- wherein R1 and R2 are independently selected from saturated or unsaturated, straight, branched and/or cyclic alkyl, aryl or aralkyl, or R1 and R2 taken together with the nitrogen atom to which they are bound form a saturated or unsaturated heterocycloalkyl.
A process for the preparation of a compound of the general formula IX:
- or a salt thereof, wherein R1 and R2 are independently selected from saturated or unsaturated, straight, branched and/or cyclic alkyl, aryl or aralkyl, or R1 and R2 taken together with the nitrogen atom to which they are bound form a saturated or unsaturated heterocycloalkyl, which process comprises the step of reacting a compound of the formula II:
- with a compound of the general formula VIII:
- wherein R1 and R2 are defined as above.
A compound of the general formula IX:
- or a salt thereof, wherein R1 and R2 are independently selected from saturated or unsaturated, straight, branched and/or cyclic alkyl, aryl or aralkyl, or R1 and R2 taken together with the nitrogen atom to which they are bound form a saturated or unsaturated heterocycloalkyl.
(canceled)
(canceled)
A method of purifying a compound of the general formula IX:
- or a salt thereof, wherein R1 and R2 are independently selected from saturated or unsaturated, straight, branched and/or cyclic alkyl, aryl or aralkyl, or R1 and R2 taken together with the nitrogen atom to which they are bound form a saturated or unsaturated heterocycloalkyl, which method comprises preparing an aqueous solution of a water-soluble salt of the compound of the general formula IX and extracting said solution with an organic solvent.
Dependencies are inferred from the claim text.