Application 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.
Solution A: To a solution of [5-methyl-3-(trifluoromethyl)-lH-pyrazol-l-yl]acetic acid (0.7 g) in dichloromethane (20 ml) at room temperature were added one drop of Nu,Nu-dimethylformamide and, dropwise, oxalyl chloride (0.8 ml). After stirring at room temperature for 2 hours, the solvent was removed and the residue was dissolved again in dichloromethane (10 ml) (solution A).To a solution of l-(2-{3-[2-(piperidin-4-yl)-l,3-thiazol-4-yl]-4,5-dihydro-l,2-oxazol-5- yl}phenyl)ethanone hydrochloride (1.20 g) in dichloromethane (20 ml) was added, at room temperature, diisopropylethylamine (1.60 ml). After 15 minutes, solution A was added dropwise. After stirring at room temperature overnight, water was added to the reaction mixture, which was extracted with ethyl acetate. The organic extracts were dried over sodium sulphate and concentrated under reduced pressure. The residue was purified by chromatography. This gave l-(4-{4-[5-(2-acetylphenyl)-4,5-dihydro-l,2- oxazol-3 -yl] – 1 ,3 -thiazol-2-yl}piperidin- 1 -yl)-2- [5 -methyl-3 -(trifluoromethyl)- lH-pyrazol- 1 -yl] ethanone (1.04 g).
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:
Patent; BAYER CROPSCIENCE AG; TSUCHIYA, Tomoki; WASNAIRE, Pierre; HOFFMANN, Sebastian; CRISTAU, Pierre; SEITZ, Thomas; KLUTH, Joachim; HILLEBRAND, Stefan; BENTING, Juergen; PORTZ, Daniela; WACHENDORFF-NEUMANN, Ulrike; WO2012/25557; (2012); A1;,
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