Electric Literature of 217448-86-7, These common heterocyclic compound, 217448-86-7, name is Methyl 1-(2,6-difluorobenzyl)-1H-1,2,3-triazole-4-carboxylate, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, such as complicated route, low yield, poor purity, etc, below Introduce a new synthetic route.
Example 8Synthesis of Compound (I)1-(2,6-Difluorobenzyl)-1H-1,2,3-triazole-4-carboxyamide (Rufinamide); 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.1H NMR (400 MHz, DMSO-d6), delta ppm: 8.56 (s, 1H), 7.87 (bs, 1H), 7.60-7.43 (m, 2H), 7.20 (m, 2H), 5.72 (s, 2H).
Statistics shows that Methyl 1-(2,6-difluorobenzyl)-1H-1,2,3-triazole-4-carboxylate is playing an increasingly important role. we look forward to future research findings about 217448-86-7.
Reference:
Patent; DIPHARMA FRANCIS S.R.L.; US2010/234616; (2010); A1;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics