1-(2-acetyl-4-fluorophenyl)pyrrolidin-2-one

反応条件: temp:0.00; pressure:0.00; stir:; See reaction.notes.procedure_details.

実験手順: 1,4-Dioxane (50 mL) was degassed by heating briefly to reflux and bubbling nitrogen gas through the solvent for 10 minutes, whilst it cooled to room temperature. CuI (180 mg, 5 mol %), glycine (284 mg, 20 mol %), 2-pyrrolidinone (1.73 mL, 22.73 mmol), K3PO4 (10.05 g, 47.35 mmol) and 1-(5-fluoro-2-iodo-phenyl)-ethanone (5.0 g, 18.94 mmol) were added sequentially to the solvent and the reaction mixture was heated at 100° C. under N2 for 10 hours. The reaction mixture was filtered through a celite plug, eluting with EtOAc and the filtrate was concentrated. The crude product was purified by flash chromatography (5% MeOH in DCM) to give the title compound (2.02 g, 48% yield) as a yellow oil 1,4-Dioxane (50 mL) was degassed by heating briefly to reflux bubbling nitrogen gas through the solvent for 10 minutes the reaction mixture was heated at 100° C. under N2 for 10 hours The reaction mixture was filtered through a celite plug eluting with EtOAc the filtrate was concentrated The crude product was purified by flash chromatography (5% MeOH in DCM)