Some common heterocyclic compound, 57946-63-1, name is 2-Bromo-4-(trifluoromethyl)aniline, molecular formula is C7H5BrF3N, 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. 57946-63-1
2-Bromo-4-(trifluoromethyl)aniline (3. 5g, 14.58 mmol), 1H-pyrazole (1 .98g, 29.2 mmol), N1,N2-dimethylethane-1,2-diamine (0.78 ml, 7.29 mmol), cesium carbonate (10.45g, 32.1 mmol) was added to degassed 1,4-dioxane (15 ml) in a sealed tube and copper(i) iodide (0.55g, 2.92 mmol) was added. The tube was sealed and heated at 120 ¡ãC for 72h. After the solution was cooled, the mixture was passed through a pad of celite and the filtrate was extracted with ethyl acetate. The ethyl acetate layer was washed withbrine, dried over Na2SO4 and concentrated. The crude was purified by column chromatography to obtain the product as off white solid (2.7g, 83percent). LCMS (ESI): mlz 228.39(M+H)+.
These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route 57946-63-1, its application will become more common.
Reference:
Patent; LUPIN LIMITED; RAMDAS, Vidya; LORIYA, Rajeshkumar, Maganlal; BANERJEE, Moloy; PATIL, Pradeep, Rangrao; JOSHI, Advait, Arun; DATRANGE, Laxmikant, Shamlal; WALKE, Deepak, Sahebrao; KHAN, Talha, Hussain; DAS, Amit, Kumar; GOTE, Ganesh, Navinchandra; KALHAPURE, Vaibhav, Madhukar; PALLE, Venkata, P.; KAMBOJ, Rajender, Kumar; (234 pag.)WO2017/37682; (2017); A1;,
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