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, 1.9 mmol), 2-fluorophenyl boronic acid (532 mg, 3.8 mmol), trans[dichlorobis(triphenylphosphine)]palladium II (266 mg, 0.38 mmol) and cesium fluoride (2.6 g, 17.1 mmol) in 150 mL degassed acetonitrile and heat at 85° C. for 2 hours. Cool the reaction, filter and purify on an SCX column, eluting with 2N ammonia/methanol. Concentrate and purify on a silica column eluting with 1 0-10% gradient of methanol/methylene chloride to give 560 mg (63%) of the title compound: mass spectrum (ion spray) m/z=470 (M+H).

1. customdegassed acetonitrile
2. temperatureCool
3. customthe reaction
4. filtrationfilter
5. custompurify on an SCX column
6. washeluting with 2N ammonia/methanol
7. concentrationConcentrate
8. custompurify on a silica column
9. washeluting with 1 0-10% gradient of methanol/methylene chloride