Synthetic Route of 1001401-62-2, Each compound has different characteristics, and only by selecting the characteristics of the compound suitable for a specific situation can the compound be applied on a large scale. 1001401-62-2, name is 2-(2H-1,2,3-Triazol-2-yl)benzoic acid, This compound has unique chemical properties. The synthetic route is as follows.
A solution of 2-(2H-1,2,3-triazol-2-yl)benzoic acid (P. Coleman, J. Schreier, WO2007/126934) (500 mg, 2.64 mmol) in SOCl2 (5 mL) was heated to refluxed for 1 hour, cooled and concentrated in vacuo. The oil was dissolved in toluene (5 mL) and added to a solution of ((3R,6R)-6-methylpiperidin-3-yl)methanol hydrochloride (M. Giradin et al, Org. Proc. Res. Dev. 2013, 17, 61-68) (437 mg, 2.65 mmol) in toluene (5 mL), then aq. sodium hydroxide (5.3 mL, 1 mol/L) was added. The mixture was stirred at 10C for 12 h, poured into water (5 mL) and extracted with EtOAc (5 mL x 3). The combined organic layers were dried over Na2SO4, filtered and concentrated in vacuo and the residue purified by chromatography on silica (petroleum ether: EtOAc =5: 1 to petroleum ether: EtOAc =1 : 1) to afford the title compound. LRMS m/z (Mu+Eta) 301.2 found, 301.2 required.
The chemical industry reduces the impact on the environment during synthesis 2-(2H-1,2,3-Triazol-2-yl)benzoic acid. I believe this compound will play a more active role in future production and life.
Reference:
Patent; MERCK SHARP & DOHME CORP.; LIVERTON, Nigel; BESHORE, Douglas C.; KUDUK, Scott D.; LUO, Yunfu; MENG, Na; YU, Tingting; WO2015/18027; (2015); A1;,
1,2,3-Triazole – Wikipedia,
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