3-[4-(TrifluoroMethoxy)phenyl]benzonitrile synthesis

Yield:-

Reaction Conditions:

with sodium carbonate;(1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride in 1,2-dimethoxyethane;water at 120; for 2 h;

Steps:

To a solution of l-bromo-4-(trifluoromethoxy)benzene (0.50 g, 2.07 mmol) in DME (6 mL) were added 3-cyanophenyl boronic acid (0.37 g, 2.49 mmol), 1,1 '- bis(diphenylphosphino)ferrocene)-dichloropalladium(II) (0.046 g, 0.062 mmol) and Na₂C0₃ (2 mL of aqueous solution, 0.44 g, 4.14 mmol). The resulting mixture was stirred at 120 °C for 2h. After removal of organic solvent, the resulting residue was dilited with water (10 mL) and extracted with methylene chloride (10 mL x 2). The organic layer was dried over MgS0₄ and concentrated in vacuo. The resulting crude residue was purified by flash column chromatography (n-hexane : ethyl acetate = 10 : 1 ratio) to give a Jl.

References:

WO2011/113606,2011,A1 Location in patent:Page/Page column 28-29