[F:1][C:2]1[CH:17]=[CH:16][CH:15]=[C:14]([F:18])[C:3]=1[CH2:4][N:5]1[CH:9]=[C:8]([C:10](OC)=O)[N:7]=[N:6]1.[NH4+:19].[OH-:20].[CH3:21]O>O>[F:18][C:14]1[CH:15]=[CH:16][CH:17]=[C:2]([F:1])[C:3]=1[CH2:4][N:5]1[CH:9]=[C:8]([CH2:10][C:21]([NH2:19])=[O:20])[N:7]=[N:6]1Methyl 1-(2,6-difluorobenzyl)-1H-1,2,3-triazole-4-carboxylate (II) (10.6 g, 41.9 mmoles), prepared as reported in Example 7, is dissolved in methanol (10 ml) and treated at room temperature under stirring with a 30% ammonia aqueous solution (40 ml), then the reaction mixture is refluxed and kept under stirring for 3 hours. The mixture is cooled to 20° C., then diluted with water, filtered, and the resulting white solid is washed with water and dried in a static dryer at 50° C. Rufinamide (8.7 g) is obtained as a crystalline white solid in 87% yield.
Wird geladen…
