These common heterocyclic compound, 16681-70-2, name is 1H-[1,2,3]Triazole-4-carboxylic acid, 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. Quality Control of 1H-[1,2,3]Triazole-4-carboxylic acid
[0784] 1H-1,2,3-triazole-5-carboxylic acid (3.4 mg, 30f.tmol) was combined with HATU (11 mg, 30 f.tmol) in DMF(0.3 mL) stirred at room temperature for 10 minutes; DIPEA(1 eq.) was added and the mixture was stirred for 1 minute.Compound 2 (10 mg, 30 f.tmol) was dissolved in DMF (0.5mL) and DIPEA (5.2 f.LL, 30 f.tmol) was added, followed byaddition of the activated acid solution. The mixture wasstirred at room temperature for 30 minutes, after which timeLCMS indicated desired product formation. Half of the crudeproduct was purified using reverse phase chromatography toyield Compound a as a TFA salt (1 mg). MS m/z [M+Htcalc’d for C26H31CIFN50 4 , 532.21. found 532. Half of thecrude product was carried to the next step without furtherpurification.
The synthetic route of 1H-[1,2,3]Triazole-4-carboxylic acid has been constantly updated, and we look forward to future research findings.
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