反应详情

温度

100 °C

A solution of palladium acetate (2.3 mg, 0.0104 mmol), 2-dicyclohexylphosphino-2′,6′-dimethoxybiphenyl (8.6 mg, 0.0209 mmol) and potassium phosphate (44.4 mg, 0.20 mmol) in water (0.040 mL) and toluene (0.150 mL) was stirred for three minutes. A solution of (4-chloro-2-fluoro-phenyl)acetic acid methyl ester (Example 40; 22.6 mg, 0.11 mmol) and 4-(4-{1-ethyl-1-[3-methyl-4-(4,4,5,5-tetramethyl-[1,3,2]dioxaborolan-2-yl)-phenyl]-propyl}-2-methyl-phenyl)-1,1,1-trifluoro-2-trifluoromethyl-butan-2-ol (Example 27-(2); 42.8 mg, 0.0747 mmol) in toluene (0.230 mL) was added, and the mixture was stirred in a nitrogen atmosphere at 100° C. for three hours. After filtration through cotton plug, the filtrate was concentrated under reduced pressure. The residue was purified by silica gel chromatography (13% ethyl acetate/hexane) to give the title compound (21.9 mg, 47%).

1. filtrationAfter filtration through cotton plug
2. concentrationthe filtrate was concentrated under reduced pressure
3. customThe residue was purified by silica gel chromatography (13% ethyl acetate/hexane)