反应详情

温度

80 °C

Dissolve trifluoromethanesulfonic acid 6-methoxy-1-[4-(2-piperidin-1-yl-ethoxy)-benzyl]-naphthalen-2-yl ester (1.50 g, 2.86 mmol) in 50 mL of acetonitrile and add 2,6-difluorophenyl boronic acid (0.90 g, 5.73 mmol), tetrakis(triphenylphosphine)palladium(0) (0.66 g, 0.57 mmol). Next add potassium phosphate (3.64 g, 17.16 mmol) and heat to 80° C. for one hour. Add Celite and filter. Concentrate the solvent under vacuum to a dark oil, dissolve in methanol and purify on an SCX cartridge, eluting with 2N ammonia/methanol. Purify further on a silica gel column eluting with a 0-10% methanol/methylene chloride gradient. Evaporate the solvent to yield 800 mg (58%) of the title compound.

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