反应详情

Dissolve trifluoromethanesulfonic acid 6-benzyloxy-1-[4-(2-piperidin-1-yl-ethoxy)-benzoyl]-naphthalen-2-yl ester (1.00 g, 1.63 mmoles) in 20 ml of acetonitrile and add 2-fluorobenzene boronic acid (0.46 g, 3.26 mmol), trans[dichlorobis(triphenylphosphine)]palladium II (0.23 gm., 0.33 mmoles) and sonicate briefly. Next add cesium fluoride (2.23 g, 14.67 mmol) and heat to 75° C. for one hour. Add Celite and filter. Concentrate the solvent under vacuum, dissolve in methanol and purify on an SCX cartridge, eluting with 2N ammonia/methanol. Further purify on a silica gel column eluting with a 0-10% methanol/methylene chloride gradient to isolate 550 mg of the title compound (60%).

1. customsonicate briefly
2. filtrationAdd Celite and filter
3. concentrationConcentrate the solvent under vacuum
4. dissolutiondissolve in methanol
5. custompurify on an SCX cartridge
6. washeluting with 2N ammonia/methanol
7. customFurther purify on a silica gel column
8. washeluting with a 0-10% methanol/methylene chloride gradient