反应详情

Charge a flask with trifluoromethanesulfonic acid 6-methoxy-1-[4-(2-piperidin-1-yl-ethoxy)-benzoyl]-naphthalen-2-yl ester (580 mg, 1.1 mmol), 2-methylsulfanyl-4-fluoro-benzene boronic acid (400 mg, 2.2 mmol) and cesium fluoride (830 mg, 5.4 mmol) and flush with nitrogen. In a separate flask, add palladium acetate (24 mg, 0.11 mmol) and tricyclohexylphosphine (62 mg, 0.22 mmol) and suspend in dry degassed acetonitrile (10 mL). Socinate under nitrogen for 10 minutes and add the catalyst solution to the solids and plunge into an 80° C. oil bath for 30 minutes. Cool to room temperature, filter through celite and concentrate in vacuo. Purify the residue by silica gel chromatography (0 to 3% methanol in methylene chloride) to yield 476 mg (83%) of the title compound: mass spectrum (ion spray) m/z=530.2 (M+H).

1. customflush with nitrogen
2. customin dry
3. customdegassed acetonitrile (10 mL)
4. additionadd the catalyst solution to the solids and plunge into an 80° C. oil bath for 30 minutes
5. filtrationfilter through celite
6. concentrationconcentrate in vacuo
7. customPurify the residue by silica gel chromatography (0 to 3% methanol in methylene chloride)