反应详情

To a solution of 125 mg (0.29 mmol) of 1-(2-hydroxy-benzyl)-4-(4-isopropyl-phenyl)-6-prop-2-ynyloxy-1H-quinazolin-2-one in acetone (5 ml) is added potassium carbonate (407 mg, 2.94 mmol) followed by 2-[2-(2-methoxy-ethoxy)-ethoxy]-ethyl-methanesulfonate (as prepared in Step A, Example RT-5) (357 mg, 1.47 mmol). The reaction mixture is heated at reflux overnight. After cooling to room temperature, the reaction mixture is quenched with water and extracted with EtOAc (2×20 ml). The combined organic layers are washed with brine, dried (Na2SO4), filtered and evaporated in vacuo to provide a yellow oil which is purified by preparative TLC chromatography on Silica gel using dichloromethane/ether (1:1) to provide the title compound as a yellow oil. Yield: 29 mg (17%).

1. temperatureThe reaction mixture is heated
2. temperatureat reflux overnight
3. customthe reaction mixture is quenched with water
4. extractionextracted with EtOAc (2×20 ml)
5. washThe combined organic layers are washed with brine
6. dry with materialdried (Na2SO4)
7. filtrationfiltered
8. customevaporated in vacuo
9. customto provide a yellow oil which
10. customis purified by preparative TLC chromatography on Silica gel