Methanol → 1-(2,6-Difluorobenzyl)-1H-1,2,3-triazole-4-carboxyamide

Participants

Reaction Conditions

Reaction Steps

Methyl 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.

Provenance & Evidence