Ethyl Acetate → 5-Bromo-2-(4-fluorophenyl)pyridine

Participants

Reaction Conditions

Reaction Steps

22.4 g (160 mmol) of 4-fluoro-benzeneboronic acid, 34 g (153.5 mmol) of 2,5-dibromopyridine and 1.24 g of tetrakis(triphenylphosphine)palladium were dissolved in 240 ml of ethanol and 480 ml of toluene. 480 ml of a 2 N sodium carbonate solution were added and the resulting mixture was heated to 50° C. with stirring for 2 h. After addition of 400 ml of ethyl acetate the mixture was filtered, the phases were separated and the organic phase was washed with a saturated sodium chloride solution, dried and evaporated. The obtained product was purified by column chromatography (silica gel, dichloromethane/heptane 1:1) and preparative HPLC (RP 18). Yield: 12 g.

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