Synthetic Route of 217448-86-7, New Advances in Chemical Research in 2021. As an important bridge between the micro and macro material world, chemistry is one of the main methods and means for humans to understand and transform the material world. 217448-86-7, name is Methyl 1-(2,6-difluorobenzyl)-1H-1,2,3-triazole-4-carboxylate, molecular formula is C11H9F2N3O2, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, below Introduce a new synthetic route.
Example 8; Synthesis 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 20C, then diluted with water, filtered, and the resulting white solid is washed with water and dried in a static dryer at 50C. 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, 1 H), 7.87 (bs, 1H), 7.60-7.43 (m, 2H), 7.20 (m, 2H), 5.72 (s, 2H).
Therefore, this conceptually novel strategy might open impressive avenues to establish green and sustainable chemistry platforms.In my other articles, you can also check out more blogs about Methyl 1-(2,6-difluorobenzyl)-1H-1,2,3-triazole-4-carboxylate.
Reference:
Patent; Dipharma Francis S.r.l.; EP2230234; (2010); A1;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics