反应详情

A mixture of 4-bromo-7-hydroxy-2-phenyl-thiazolo[5,4-c]pyridine-6-carboxylic acid ethyl ester (230 mg, 0.61 mmole), 4-morpholinophenylboronic acid (252 mg, 1.22 mmole), cesium carbonate (596 mg, 1.83 mmole) and tetrakis(triphenylphosphine)-palladium (70 mg, 0.06 mmole) in dioxane (3 ml) was refluxed for 18 h before it was cooled to room temperature, quenched with water and filtered. The filtrate was partitioned between ethyl acetate and water. The organic layer was washed with brine, dried over anhydrous sodium sulfate and concentrated in vacuo. The residue was purified by flash column chromatography on silica gel with a gradient of ethyl acetate and dichloromethane to give the title compound as a white solid (57 mg). MS: (+) m/z 462.35 (M+H+)

1. temperaturewas refluxed for 18 h before it
2. customquenched with water
3. filtrationfiltered
4. customThe filtrate was partitioned between ethyl acetate and water
5. washThe organic layer was washed with brine
6. dry with materialdried over anhydrous sodium sulfate
7. concentrationconcentrated in vacuo
8. customThe residue was purified by flash column chromatography on silica gel with a gradient of ethyl acetate and dichloromethane