反应详情

1-(3-Bromo-phenyl)-3-(2-naphthalen-1-yl-2H-pyrazol-3-yl)-1H-pyridazin-4-one (example 190) (100 mg, 0.23 mmol) was dissolved in EtOAc (3 ml) and the solution was placed in the reaction vessel. [PdCl2(dppf)] (10 mg) was added followed by 2-fluoroethanol (97 mg, 1.5 mmol) and Et3N (0.05 ml). The reactor was closed and the mixture was stirred 20 h under 70 bar carbon monoxide at 110° C. After evaporation of the solvents the residue was purified by chromatography (10 g SiO2, Hept to Hept/EtOAc 1:1). The product was isolated as an off-white solid (69 mg, 67%). MS: M=455.1 (M+H)+

1. customThe reactor was closed
2. customAfter evaporation of the solvents the residue
3. customwas purified by chromatography (10 g SiO2, Hept to Hept/EtOAc 1:1)