反应详情

温度

80 °C

Add trifluoromethanesulfonic acid 6-methoxy-1-[4-(2-piperidin-1-yl-ethoxy)-benzoyl]-naphthalen-2-yl ester (552 mg, 1.0 mmol), 2,6-difluorophenyl boronic acid (320 mg, 2.0 mmol), trans dichlorobis(triphenylphosphine)palladium II (70 mg, 0.1 mmol) and cesium fluoride (1.3 g, 8.6 mmol) to a 20 mL vial along with 8.0 mL degassed acetonitrile. Seal the vial with a septum and purge with nitrogen gas. Heat the mixture with stirring at 80° C. for three hours. Cool, filter and purify on an SCX column, eluting with 2N ammonia/methanol. The compound is further purified on a silica gel column, eluting with a 0-5% 2N ammonia in methanol/methylene chloride gradient. The yield is 260 mg (50%).

1. customdegassed acetonitrile
2. customSeal the vial with a septum
3. custompurge with nitrogen gas
4. temperatureHeat the mixture
5. temperatureCool
6. filtrationfilter
7. custompurify on an SCX column
8. washeluting with 2N ammonia/methanol
9. customThe compound is further purified on a silica gel column
10. washeluting with a 0-5% 2N ammonia in methanol/methylene chloride gradient