Some common heterocyclic compound, 16681-70-2, name is 1H-[1,2,3]Triazole-4-carboxylic acid, molecular formula is C3H3N3O2, 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. Recommanded Product: 1H-[1,2,3]Triazole-4-carboxylic acid
[0838] lH-1,2,3-triazole-4-carboxylic acid (2.3 mg, 20f.tmol) was combined with HATU (7.7 mg, 20 flillOl) in DMF(2 mL) and stirred at room temperature for 15 minutes. Compound3(7.7 mg, 18 flillOl) andDIPEA(9.6 f.LL, 55 f.tmol)werethen added. The solution was stirred at room temperature for15 minutes, at which time LCMS showed reaction completion.The solvent was removed in vacuo and the crude residuewas dissolved in EtOH (2 mL). A solution of IN LiOH (183f.LL, 183 f.tmol) in water was added, and the resulting solutionwas stirred at room temperature for 30 minutes, at which timeLCMS showed reaction completion. The solvent wasremoved in vacuo and the crude residue was purified byreverse phase chromatography to yield Compound a (3 mg) asa TFA salt. MS m/z [M+Ht calc’d for C23H25ClFN50 4 ,490.16. found 488.
These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route 16681-70-2, its application will become more common.
Reference:
Patent; THERAVANCE BIOPHARMA R&D IP, LLC; Fleury, Melissa; Beausoliel, Anne-Marie; Hughes, Adam D.; Long, Daniel D.; Wilton, Donna A.A.; US2015/210690; (2015); A1;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics