Related Products of 458-50-4, These common heterocyclic compound, 458-50-4, name is 4-Bromo-3-fluoroanisole, 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.
Step A1, 1 -dimethylethyl 4-[2~fluoro~4-(methyloxy)phenyl]-3-oxo-1-piperazinecarboxylate A mixture of 1-Boc-3-oxopiperazine (500 mg, 2.497 mmol), 4-bromo-3- fluoroanisole (512 mg, 2.497 mmol), copper(l) iodide (23.78 mg, 0.125 mmol), frans-Nu,Nu’- dimethylcycIohexane-1 ,2-diamine (0.039 mL, 0.250 mmo.), and potassium carbonate (690 mg, 4.99 mmol) in 1 ,4-dioxane (10 mL) was heated at 120 °C for 3.5 days. The mixture was filtered through a pad of Celite and washed with EtOAc (50 mL). The filtrate was washed with saturated aqueous NH4CI (15 mL), brine (15 mL), dried ( gS04), filtered and concentrated. The crude was absorbed on silica gel and purified by silica gelchromatography (10-60percent EtOAc in hexanes) to give 1 ,1 -dimethylethyl 4-[2-fluoro-4- (methyloxy)phenyl]-3-oxo~1 -piperazinecarboxylate (581.9 mg, 1 .794 mmol, 72 percent) as white solid. MS(ESI) m/z: 325.3 (MH+).
Statistics shows that 4-Bromo-3-fluoroanisole is playing an increasingly important role. we look forward to future research findings about 458-50-4.