反应详情

温度

80 °C

A mixture of Compound 1c (50 mg, 0.206 mmol), 4-bromo-2,6-difluoroanisole (45.9 mL, 0.206 mmol), bis(triphenylphosphine)palladium(II)dichloride (7.23 mg, 0.012 mmol), CuI (3.92 mg, 0.206 mmol) in anhydrous and degassed triethylamine (3 mL) was heated at 80° C. under a nitrogen atmosphere for 2 h in a sealed vessel. The reaction mixture was cooled, filtered on Celite, poured into water and extracted with EtOAc. The combined organic layers were washed with brine, dried on Na2SO4 and evaporated to dryness in vacuo to afford a residue, which was purified by flash chromatography (EtOAc—Petroleum Ether 10:90) affording the title product (22 mg).

1. customdegassed triethylamine (3 mL)
2. temperatureThe reaction mixture was cooled
3. filtrationfiltered on Celite
4. additionpoured into water
5. extractionextracted with EtOAc
6. washThe combined organic layers were washed with brine
7. customdried on Na2SO4
8. customevaporated to dryness in vacuo
9. customto afford a residue, which
10. customwas purified by flash chromatography (EtOAc—Petroleum Ether 10:90)