反应详情

温度

85 °C

Dissolve trifluoromethanesulfonic acid 6-methoxy-1-[4-(2-piperidin-1-yl-ethoxy)-benzyl]-naphthalen-2-yl ester (1.0 g, 1.91 mmol), 4-fluorophenyl boronic acid (3.8 g., 3.8 mmol), trans[dichlorobis(triphenylphosphine)]palladium II (266 mg, 0.38 mmol) and cesium fluoride (2.6 g, 17.1 mmol) in 125 mL degassed acetonitrile and heat at 85° C. for 8 hours. Cool and filter and purify on an SCX column and elute with 2 N ammonia/methanol. Evaporate to an oil and purify on a silica gel column eluting with a gradient of 0-10% methanol/methylene chloride: mass spectrum (ion spray) m/z=470 (M+H).

1. customdegassed acetonitrile
2. temperatureCool
3. filtrationfilter
4. custompurify on an SCX column
5. washelute with 2 N ammonia/methanol
6. customEvaporate to an oil
7. custompurify on a silica gel column
8. washeluting with a gradient of 0-10% methanol/methylene chloride