反应详情

A solution of 4-(6-chloro-2-(4-fluoro-1H-indol-2-yl)pyridin-3-yl)but-3-en-1-ol (500 mg, 1.58 mmol), (2-(4-fluorophenyl)-3-(methylcarbamoyl)-6-(N-methylmethyl sulfonamido)benzofuran-5-yl)boronic acid (800 mg, 1.89 mmol) and Na2CO3 (340 mg, 3.15 mmol) in dioxane/DMF/H2O (5 mL/1 mL/0.2 mL) was added Pd2(dba)3 (10 mg) and X-Phos (10 mg) under N2. It was put into a pre-heated oil-bath at 110° C. for 8 hours. The mixture was concentrated and it was extracted with EtOAc. The combined organic phase was washed with brine, and dried over Na2SO4. The crude product was purified by column (PE:EA=1:1) to give the pure product of (Z and E)-5-(6-(4-fluoro-1H-indol-2-yl)-5-(4-hydroxybut-1-en-1-yl)pyridin-2-yl)-2-(4-fluorophenyl)-N-methyl-6-(N-methylmethylsulfonamido)benzofuran-3-carboxamide (570 mg, yield: 52%).

1. concentrationThe mixture was concentrated
2. extractionit was extracted with EtOAc
3. washThe combined organic phase was washed with brine
4. dry with materialdried over Na2SO4
5. customThe crude product was purified by column (PE:EA=1:1)