Synthetic Route of 288-36-8, New Advances in Chemical Research in 2021. The dynamic chemical diversity of the numerous elements, ions and molecules that constitute the basis of life provides wide challenges and opportunities for research. 288-36-8, name is 1H-1,2,3-Triazole, molecular formula is C2H3N3, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, below Introduce a new synthetic route.
In a dry Schlenk Tube at RT under nitrogen are successively charged 2-fluoro-6-iodo-3- methyl-benzoic acid (1.786 mmol, 1 eq), Cul (0.089 mmol, 0.05 eq), 1 H-1 ,2,3-triazole (3.571 mmol, 2 eq), Cs2C03 (3.571 mmol, 2 eq) and DMF (2.5 mL). The resulting blue suspension is stirred at 80C overnight. The obtained reaction mixture is taken up in 1 M aq. HCI and extracted twice with EtOAc. The combined organic layers are dried over Na2S04, filtered and concentrated under reduced pressure. Purification is achieved by preparative HPLC (conditions D) to give the titled compound (246 mg) as a pale yellow solid. LC-MS (conditions A): tR = 0.55 min, [M + 1 ]+ = 222.19.
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Reference:
Patent; ACTELION PHARMACEUTICALS LTD; BOSS, Christoph; BROTSCHI, Christine; HEIDMANN, Bibia; SIFFERLEN, Thierry; WILLIAMS, Jodi T.; WO2012/85857; (2012); A1;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics