Synthetic Route of 51776-71-7, A common heterocyclic compound, 51776-71-7, name is 1-Bromo-4-(difluoromethyl)benzene, molecular formula is C7H5BrF2, 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.
A stirred mixture of l-bromo-4-(difluoromethyl)benzene (0.76 g, 3.7 mmol), bis(pinacolato)diboron (1.13 g, 4.4 mmol), l,l’-bis(diphenylphosphino)ferrocene- palladium dichloride (0.31 g, 0.37 mmol), and potassium acetate (1.09 g, 11.1 mmol) in dry 1,4-dioxane (10.0 mL) was purged three times with argon and placed under vacuum three times. The mixture was heated to 90 C and monitored with LC-MS and TLC. After 21 h, the reactions were cooled to rt then filtered through Celite. The organic solvent was removed under reduced pressure, and the residue was purified on silica gel (0-10% EtOAc in hexanes) to yield a yellow liquid as 2-(4-(difluoromethyl)phenyl)-4,4,5,5-tetramethyl-l,3,2- dioxaborolane. 1H NMR (400 MHz, DMSO-d6) delta ppm 7.80 (2 H, m, J=8.0 Hz), 7.57 (2 H, m, J=8.0 Hz), 7.05 (1 H, t), 1.36 (12 H, s).
The synthetic route of 51776-71-7 has been constantly updated, and we look forward to future research findings.
Reference:
Patent; AMGEN INC.; DRANSFIELD, Paul, John; GONZALEZ LOPEZ DE TURISO, Felix; KOHN, Todd, J.; PATTAROPONG, Vatee; SIMARD, Jillian, L.; WO2012/3283; (2012); A1;,
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