Electric Literature of 345637-71-0,Some common heterocyclic compound, 345637-71-0, name is 2-(5-Methyl-3-(trifluoromethyl)-1H-pyrazol-1-yl)acetic acid, molecular formula is C7H7F3N2O2, 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.
Oxalylchloride (0.32 g, 2.6 mmol) and then one drop of N,Ndimethylformamidewere consecutively added to a solution of (5-methyl-3-trifluoromethyl-pyrazol-1-yl)-acetic acid (0.45 g, 2.1 mmol) in 8 ml ofdichloromethane. The resulting mixture was stirred for 16 h at room temperatureand evaporated under reduced pressure. The residue was dissolved in 5 ml ofdichloromethane and added to a solution of ethyl 2-[2-(methylamino)ethyl]thiazole-4-carboxylate (23b, 0.65 g, 2.6 mmol) andtriethylamine (1.0 g, 10 mmol) in 5 ml of dichloromethane. The reaction mixturewas stirred for 4 h at room temperature, then diluted with water and extractedwith dichloromethane. The organic layer was washed with water and brine,dried over sodium sulfate and evaporated under reduced pressure, the remainderwas purified by chromatography on silica gel, using ethyl acetate / cyclohexane1 : 1 as eluent system to obtain ethyl 2-[2-[methyl-[2-[5-methyl-3-(trifluoromethyl)pyrazol-1-yl]acetyl]amino]ethyl] thiazole-4-carboxylate (24b,0.39 g, 1.0 mmol, 44 %).
These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route 2-(5-Methyl-3-(trifluoromethyl)-1H-pyrazol-1-yl)acetic acid, its application will become more common.
Reference:
Article; Sulzer-Mosse, Sarah; Lamberth, Clemens; Kubizna, Peter; Synlett; vol. 28; 17; (2017); p. 2277 – 2280;,
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