反应详情

Combine trifluoromethanesulfonic acid 1-formyl-6-methoxy-naphthalen-2-yl ester (2.53 g, 7.6 mmol) with dichlorobis(triphenylphosphine)palladium (II) (0.53 g, 0.8 mmol), cesium fluoride (5.75 g, 37.8 mmol), and 2,4-difluorophenylboronic acid (2.39 g, 15.1 mmol) in acetonitrile (25 mL). Heat to reflux for 1 hour. Cool to room temperature, add DARCO, and filter. Concentrate in vacuo, dilute with dichloromethane and wash with saturated aqueous sodium carbonate. Dry the organic layer over magnesium sulfate, filter, add silica gel, and concentrate in vacuo. Purify the residue by column chromatography using an eluent of 1.5:1 hexanes:dichloromethane to give 1.4 g of the title compound (62%).

1. temperatureHeat
2. temperatureto reflux for 1 hour
3. filtrationfilter
4. concentrationConcentrate in vacuo
5. additiondilute with dichloromethane
6. washwash with saturated aqueous sodium carbonate
7. dry with materialDry the organic layer over magnesium sulfate
8. filtrationfilter
9. additionadd silica gel
10. concentrationconcentrate in vacuo
11. customPurify the residue by column chromatography