反应详情

温度

85 °C

To a solution of 3-phenyl-5-bromo-1-(phenylsulfonyl)-1H-pyrrolo[2,3-b]pyridine (309 mg, 0.75 mmol) in a 3:1 toluene/ethanol mixture (24 ml) are added 2-methoxy-benzene boronic acid (125 mg, 0.83 mmol), K2CO3 (2.4 ml of 2 M solution in water, 4.5 mmol), Pd(PPh3)4 (1.5 mol %), and the mixture is heated at 85° C. for 2 hours under argon. The mixture is cooled to room temperature, concentrated under a vacuum and redissolved in a water/CH2Cl2 mixture. The aqueous phase is extracted several times with CH2Cl2 and the combined organic phases are dried on MgSO4. The solvent is evaporated under reduced pressure and the residue purified by flash chromatography on silica gel (100% CH2Cl2) to yield the purified product in the form of a colorless oil with a yield of 98%.

1. temperatureThe mixture is cooled to room temperature
2. concentrationconcentrated under a vacuum
3. dissolutionredissolved in a water/CH2Cl2 mixture
4. extractionThe aqueous phase is extracted several times with CH2Cl2
5. customthe combined organic phases are dried on MgSO4
6. customThe solvent is evaporated under reduced pressure
7. customthe residue purified by flash chromatography on silica gel (100% CH2Cl2)
8. customto yield the purified product in the form of a colorless oil with a yield of 98%