HRID630511
反应详情
EQUATION
反应方程式
REACTANTS
反应物
PRODUCTS
生成物
AUXILIARIES
试剂、催化剂与溶剂
CONDITIONS
反应条件
- 温度
- 90 °C
PROCEDURE
实验过程
Bis(tri-tert-butylphosphine) palladium(0)(0.51 g, 1.0 mmol) was added under an argon atmosphere to a suspension of [1-(5-bromo-pyrimidin-2-yl)-3-methanesulfinyl-1H-indol-6-yl]-morpholin-4-yl-methanone (1.0 g, 2.0 mmol), 2-fluoro-5-hydroxyphenylboronic acid (0.625 g, 4.0 mmol) and potassium fluoride (0.29 g, 5.0 mmol) in dioxane (50 ml). The reaction mixture was stirred at 90° C. for 4 h and then filtered through a pad of celite. The filter was washed with dichloromethane (2×20 mL) and concentrated. The residue was purified by flash column chromatography [silica; dichloromethane with 2% methanol]. Light yellow solid. Yield: 0.44 g (46% of theory)
WORKUP
后处理
- filtrationfiltered through a pad of celite
- washThe filter was washed with dichloromethane (2×20 mL)
- concentrationconcentrated
- customThe residue was purified by flash column chromatography [silica; dichloromethane with 2% methanol]