Application of 261762-35-0,Some common heterocyclic compound, 261762-35-0, name is 5-Bromo-1,2-difluoro-3-methoxybenzene, molecular formula is C7H5BrF2O, 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.
3,4-Difluoro-5-methoxybenzoic acid (72a) (0327) The title compound was prepared by reaction of 5-bromo-1,2-difluoro-3-methoxybenzene (1.03 g, 4.62 mmol, 1.0 equiv) and magnesium (112 mg, 4.61 mmol, 1.0 equiv) and iodine (2 mg) in 13 ml diethylether under reflux for 2 h. Carbon dioxide was bubbled through the solution at 10 C. until all solvent (13 ml) was evaporated two times. The crude product was dissolved in 10 mL THF and carbon dioxide was bubbled through the solution for additional 1 h. The reaction was quenched with 1 M HCl, extracted with ethyl acetate, dried with magnesium sulfate and concentrated under reduced pressure to afford the crude product, which was purified by flash chromatography; yield: 31% (265 mg). 1H NMR (300 MHz, MeOH-d4) delta 7.65-7.45 (m, 2H), 3.99 (s, 1H).
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-1,2-difluoro-3-methoxybenzene, its application will become more common.
Reference:
Patent; ELEXOPHARM GMBH; Hartmann, Rolf; Frotscher, Martin; Ahmed, Ahmed Saad Abdelsamie; Bey, Emmanuel; van Koppen, Chris J.; Oberwinkler-Marchais, Sandrine; Boerger, Carsten; Siebenbuerger, Lorenz; Hernandez Olmos, Victor; (72 pag.)US2016/318895; (2016); A1;,
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