反应详情

温度

125 °C

To a solution of compound 5 (1.0 g, 2.61 mmol) in dioxane (12 mL) at room temperature was added dropwise a solution of Cs2CO3 (2.5 g, 7.66 mmol) in water (3 mL), followed by addition of Pd(PPh3)4 (300 mg, 0.26 mmol) and 4-(4,4,5,5-Tetramethyl-[1,3,2]dioxaborolan-2-yl)-3,6-dihydro-2H-pyran (636 mg, 3.0 mmol). The reaction mixture was degassed by purging with N2 for 15 min. Then the mixture was heated to 125° C. under microwave irradiation for 40 min. After removal the solvent, the residue was purified by chromatography on silica gel column eluted with PE/EtOAc=10:1 to 1:5) to afford compound 6 (680 mg, 76% yield) as a white solid. LC-MS: m/z 339.1 [M+H]+.

1. customThe reaction mixture was degassed
2. customby purging with N2 for 15 min
3. customAfter removal the solvent
4. customthe residue was purified by chromatography on silica gel column
5. washeluted with PE/EtOAc=10:1 to 1:5)