反应详情

To a solution of methyl 2-bromo-1-(2-tert-butoxy-2-oxoethyl)-3-cyclohexyl-1H-indole-6-carboxylate in 1,4-dioxane (0.15 M) was added Na2CO3 (6 eq, 2 M solution), (2-formylphenyl)boronic acid (1.5 eq) and bis(triphenylphosphine)palladium(II) dichloride (0.2 eq) and the mixture heated at reflux for 45 min. The reaction mixture was allowed to cool and filtered. The filtrate was diluted with EtOAc and the organic phase washed with H2O, brine and dried over Na2SO4 before being filtered and concentrated in vacuo. The crude material was purified by flash chromatography (1:9 EtOAc/PE) to afford the title compound as a yellow solid (53%); MS (ES+) m/z 476 (M+H)+

1. temperaturethe mixture heated
2. temperatureat reflux for 45 min
3. temperatureto cool
4. filtrationfiltered
5. additionThe filtrate was diluted with EtOAc
6. washthe organic phase washed with H2O, brine
7. dry with materialdried over Na2SO4
8. filtrationbefore being filtered
9. concentrationconcentrated in vacuo
10. customThe crude material was purified by flash chromatography (1:9 EtOAc/PE)