反应详情

To a solution of methyl 2-bromo-3-cyclohexyl-1-(3-methoxy-3-oxopropyl)-1H-indole-6-carboxylate in dioxane (0.15 M) was added Na2CO3 (4 eq, 2 M aqueous solution), tert-butyl [2-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl]carbamate (1.5 eq) and bis(triphenylphosphine)palladium(II) dichloride (0.2 eq). The mixture was heated at reflux for 45 mins. The reaction mixture was filtered and then the filtrate was diluted with EtOAc. The organic phase was washed with H2O, brine and dried over Na2SO4 before being filtered and concentrated in vacuo. The crude was purified by flash chromatography (Biotage cartridge Si65i, 1:9 EtOAc/PE) to give the title compound as a white solid (60%); MS (ES+) m/z 535 (M+H)+.

1. temperatureThe mixture was heated
2. temperatureat reflux for 45 mins
3. filtrationThe reaction mixture was filtered
4. additionthe filtrate was diluted with EtOAc
5. washThe organic phase was washed with H2O, brine
6. dry with materialdried over Na2SO4
7. filtrationbefore being filtered
8. concentrationconcentrated in vacuo
9. customThe crude was purified by flash chromatography (Biotage cartridge Si65i, 1:9 EtOAc/PE)