反应详情

温度

110 °C

To a solution of 1-benzyl-4-piperazin-1yl-phthalazine (100 mg, 0.329 mmol) in 1 mL THF is added 4-bromo-benzotrifluoride (99 mg, 0.443 mmol), potassium tert-butoxide (55.3 mg, 0.493 mmol), XPhos [2-(Dicyclohexylphosphino)-2′,4′,6′-tri-1-propyl-1′-1′-biphenyl] (15.7 mg, 0.033 mmol), and palladium (II) acetate (11 mg, 0.16 mmol) in a 2 dram screw-top vial. The vial is evacuated and flushed with argon. The reaction mixture was heated to 110° C. for 18 hrs. The mixture is then poured into water (50 mL), and the precipitate is isolated by filtration. The resulting solid is purified by flash chromatography on silica gel (10-70% EtOAc:heptanes) to provide the desired product as yellow crystals (54 mg, 37% yield).

1. customThe vial is evacuated
2. customflushed with argon
3. additionThe mixture is then poured into water (50 mL)
4. customthe precipitate is isolated by filtration
5. customThe resulting solid is purified by flash chromatography on silica gel (10-70% EtOAc:heptanes)