Synthetic Route of 16681-70-2, New Advances in Chemical Research in 2021. The transformation of simple hydrocarbons into more complex and valuable products via catalytic C–H bond functionalisation has revolutionised modern synthetic chemistry. 16681-70-2, name is 1H-[1,2,3]Triazole-4-carboxylic acid, molecular formula is C3H3N3O2, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, below Introduce a new synthetic route.
Compound 3 (30 mg, 199 muiotaetaomicron) was combined with 3H-[l,2,3]triazole-4- carboxylic acid (22 mg, 199 muiotaetaomicron), HATU (76 mg, 199 muiotaetaomicron) and DIPEA (104 mu, 596 muiotaetaomicron) in DMF (1 mL) and stirred at room temperature for 20 minutes then concentrated in vacuo and the crude residue was purified by normal phase chromatography (0-100% EtOAc/hexanes). The intermediate (30 mg, 67 muiotaetaomicron) was dissolved in THF (1 mL) and 10N NaOH (268 mu^, 268 muiotaetaomicron) and stirred at room temperature for 1 hour. The mixture was acidified with AcOH and purified by preparative HPLC to yield Compound 4 (10 mg).
The result showed that such a combination of chemo- and biocatalysis improved the catalytic yield more than two times compared with that of sole metal catalysis.I hope my blog about 1H-[1,2,3]Triazole-4-carboxylic acid is helpful to your research.
Reference:
Patent; THERAVANCE BIOPHARMA R&D IP, LLC; FLEURY, Melissa; BEAUSOLIEL, Anne-Marie; HUGHES, Adam D.; LONG, Daniel D.; WILTON, Donna A.A.; WO2015/116786; (2015); A1;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics