These common heterocyclic compound, 886762-08-9, name is 5-Bromo-2-(trifluoromethoxy)aniline, its 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. Recommanded Product: 5-Bromo-2-(trifluoromethoxy)aniline
General procedure: To a solution of N-tosylhydrazone (0.6mmol, 1.1 eq) in distilled dioxane (8mL) was added bis(acetonitrile)palladium(II) chloride (0.05mmol, 5mol %), and dppp (0.1mmol, 10mol %). The resulting suspension was stirred RT for 2min, and cesium carbonate (1.5mmol, 3.0 eq) was added. Then, the reaction mixture was stirred for additional 2min, and aryl bromide (0.5mmol, 1.0 eq) was added in one portion. The mixture was then heated at 100C for 3h. The crude reaction mixture was allowed to cool to rt. EtOAc was added, and the mixture was filtrated through Celite. The solvent was evaporated under reduced pressure, and the crude product was purified by flash chromatography on silica gel.
The synthetic route of 5-Bromo-2-(trifluoromethoxy)aniline has been constantly updated, and we look forward to future research findings.
Reference:
Article; Naret, Timothee; Bignon, Jerome; Bernadat, Guillaume; Benchekroun, Mohamed; Levaique, Helene; Lenoir, Christine; Dubois, Joelle; Pruvost, Alain; Saller, Francois; Borgel, Delphine; Manoury, Boris; Leblais, Veronique; Darrigrand, Romain; Apcher, Sebastien; Brion, Jean-Daniel; Schmitt, Etienne; Leroux, Frederic R.; Alami, Mouad; Hamze, Abdallah; European Journal of Medicinal Chemistry; vol. 143; (2018); p. 473 – 490;,
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