Introduction of a new synthetic route about 4-Bromo-3-fluoroanisole

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458-50-4, Each compound has different characteristics, and only by selecting the characteristics of the compound suitable for a specific situation can the compound be applied on a large scale. 458-50-4, name is 4-Bromo-3-fluoroanisole, This compound has unique chemical properties. The synthetic route is as follows.

Into the solution of l-bromo-2-fluoro-4-methoxybenzene (1000 g, 4.88 mol, 1.00 equiv) in tetrahydrofuran (10 L) was added drop wise LDA (2561 mL, 1.05 equiv) at -78 ¡ãC under nitrogen. The resulting solution was stirred for Ih at -70 ¡ãC. Then to the above solution, (Z)-N-[(tert-butoxy)carbonyI]imino(tert-butoxy)fomamide (1 122 g, 4.87 mol, 1.00 equiv.) was added. The resulting solution was stirred for 1 h at -78 ¡ãC, The reaction was then quenched by the addition of 200 mL of methanol. The resulting mixture was concentrated under vacuum and dissolved in EA (6L) , washed with water (2L) for two times and organic layers concentrated under vacuum. This resulted in 1400 g (66percent) of the title compound as a white solid.

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Reference:
Patent; EPIZYME, INC.; CAMPBELL, John Emmerson; DUNCAN, Kenneth William; MILLS, James Edward John; MUNCHHOF, Michael John; (301 pag.)WO2019/79540; (2019); A1;,
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