反应详情

温度

70 °C

To a solution of (1-(6-bromo-2-chloropyridin-3-yl)cyclopropyl)methanol (100 mg, 0.381 mmol) and (2-(4-fluorophenyl)-3-(methylcarbamoyl)-6-(N-methylmethylsulfonamido)benzofuran-5-yl)boronic acid (160 mg, 0.381 mmol) in 1,4-Dioxane (2 mL) and water (20 μL) was added K2CO3 (105 mg, 0.762 mmol) and Pd(dppf)Cl2 (55 mg, 0.075 mmol). The mixture was heated to 70° C. and stirred overnight. Filtration through a pad of celite removed the solid. After washing with ethyl acetate, the combined filtrate was concentrated in vacuo. Preparative TLC gave 5-(6-chloro-5-(1-(hydroxymethyl)cyclopropyl)pyridin-2-yl)-2-(4-fluorophenyl)-N-methyl-6-(N-methylmethylsulfonamido)benzofuran-3-carboxamide (80 mg, yield: 37.6%) MS (M+H)+: 559.

1. filtrationFiltration through a pad of celite
2. customremoved the solid
3. washAfter washing with ethyl acetate
4. concentrationthe combined filtrate was concentrated in vacuo