反应详情

温度

100 °C

1.6 g 2-(Trifluormethyl)pyridin-5-ylboronic acid, 1.66 g commercially available 5-Bromo-2,3-dihydro-1H-indole and 8.19 g cesium carbonate were dissolved in a mixture of 7 ml water and 21 ml dimethylformamide. The reaction mixture was degassed with argon and then 484 mg tetrakis(triphenylphosphine)palladium(0) were added and the mixture heated to 100° C. for two hours. The cooled reaction mixture was diluted with 200 ml ethyl acetate and washed with 100 ml water and brine. The organic layer was dried over MgSO4 and the solvent removed in vacuo. The resulting crude material was purified by purified by chromatography on silica gel to obtain 885 mg 5-(6-Trifluoromethyl-pyridin-3-yl)-2,3-dihydro-1H-indole.

1. customThe reaction mixture was degassed with argon
2. addition484 mg tetrakis(triphenylphosphine)palladium(0) were added
3. customThe cooled reaction mixture
4. washwashed with 100 ml water and brine
5. dry with materialThe organic layer was dried over MgSO4
6. customthe solvent removed in vacuo
7. customThe resulting crude material was purified
8. customby purified by chromatography on silica gel