Synthetic Route of 627871-16-3,Some common heterocyclic compound, 627871-16-3, name is 5-Bromo-4-fluoro-2-methylaniline, molecular formula is C7H7BrFN, 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.
Under a nitrogen atmosphere, 5-bromo-4-fluoro-2-methylaniline (2.0 g, 9.80 mmol),Bis (pinacolato) diboron (3.73 g, 14.7 mmol),Palladium acetate (220 mg, 0.98 mmol),X-Phos (701 mg, 1.47 mmoll) and potassium acetate (2.89 g, 29.4 mmol) were suspended in 1,4-dioxane (20 mL),Under heating reflux,Stir for 1.5 hours.It was allowed to cool, diluted with water, and extracted with ethyl acetate.Wash the organic layer with saturated saline,Dried over anhydrous magnesium sulfate,The solvent was distilled off under reduced pressure.The obtained residue was purified by silica gel column chromatography (hexane-ethyl acetate),Compound 14(1.65g,Yield 67.0%).
These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route 5-Bromo-4-fluoro-2-methylaniline, its application will become more common.
Reference:
Patent; Shionogi Co Ltd; Ogawa, Tomoyuki; (39 pag.)JP2019/182806; (2019); A;,
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