Extended knowledge of 4-[1,2,4]Triazol-1-yl-benzoic acid

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162848-16-0, Researchers who often do experiments know that organic synthesis is a process of preparing more complex target molecules from simple raw materials through one or more chemical reactions. Generally, it requires fewer steps, and cheap raw materials. 162848-16-0, name is 4-[1,2,4]Triazol-1-yl-benzoic acid, A new synthetic method of this compound is introduced below.

At 40 C 1-hydroxybenzotriazole hydrate (0.13 g, 0.99 mmol) and 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride (0.19 g, 0.99 mmol) were added to astirred solution of 4-(1/-/-1,2,4 triazol-1yl)benzoic acid (0.16 g, 0.82 mmol) in N,N-dimethylformamide (5 mL). After 30 minutes methyl-phenyl-carbamic acid 5-amino-pyridin-2-yl ester (0.20 g, 0.82 mmol) and A/-ethyldiisopropylamine (0.17 mL, 0.99 mmol) were addedand stirring was continued overnight at 40 C. The solvent was evaporated in vacuo. A smallportion of the crude product (around 100 mg) was purified by preparative HPLC yielding thetitle compound (10 mg. 1% yield) as a white solid.1H NMR (400 MHz, DMSO-c/6): 5- 7.25 (d, 1H), 7.30 (m, 1H), 7.45 (m, 4H), 8.07 (d,2H), 8.18 (d, 2H), 8.28 (dd, 1H), 8.32 (s, 1H), 8.69 (d, 1H), 9.45 (s, 1H), 10.62 (s, 1H); HPLC-MS (Method A): m/z = 415 (M+H)+; Rt = 3.13 min.

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Reference:
Patent; NOVO NORDISK A/S; WO2004/111031; (2004); A1;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics