反应详情

温度

-78 °C

To a solution of 8-chloro-1-(2-fluoro-4-iodophenyl)-5-methyl-3,5-dihydrodiimidazo[4,5-b:4′,5′-e]pyridin-2(1H)-one (200 mg, 0.36 mmol) in THF (6 ml) at −78° C. is added LiHMDS (0.54 ml, 1 M in THF, 0.54 mmol). The reaction mixture is stirred at −78° C. for 10 min and cyclopropylsulfonyl chloride (100 mg, 0.72 mmol) is added to the mixture. The reaction is slowly warmed to room temperature and stirred at the temperature for 3 h. The reaction is quenched with saturated aqueous NH4Cl solution (10 ml) and extracted with EtOAc (2×10 ml). The combined organic solution is washed with brine (10 ml), dried over MgSO4 and concentrated. Silica gel chromatography yields the title compound.

1. temperatureThe reaction is slowly warmed to room temperature
2. stirringstirred at the temperature for 3 h
3. customThe reaction is quenched with saturated aqueous NH4Cl solution (10 ml)
4. extractionextracted with EtOAc (2×10 ml)
5. washThe combined organic solution is washed with brine (10 ml)
6. dry with materialdried over MgSO4
7. concentrationconcentrated