反应详情

温度

100 °C

A solution of palladium acetate (3.4 mg, 0.015 mmol), 2-dicyclohexylphosphino-2′,6′-dimethoxybiphenyl (12.3 mg, 0.03 mmol) and potassium phosphate (63.7 mg, 0.3 mmol) in water (0.045 mL) and toluene (0.200 mL) was stirred for three minutes. A solution of (4-chloro-2-fluoro-phenyl)acetic acid methyl ester (Example 40; 32.6 mg, 0.16 mmol) and 2-(4-{1-ethyl-1-[3-methyl-4-(1-trimethylsilanyloxy-cyclopentylethynyl)-phenyl]-propyl}-2-methyl-phenyl)-4,4,5,5-tetramethyl-[1,3,2]dioxaborolane (Example 32-(4); 60.0 mg, 0.10 mmol) in toluene (0.25 mL) was added, and the mixture was stirred in a nitrogen atmosphere at 100° C. for one hour. After filtration through cotton plug, the filtrate was concentrated under reduced pressure. The residue was purified by thin layer silica gel chromatography (3% ethyl acetate/hexane) to give the title compound (52.6 mg, 81%).

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