反应详情

To a solution of 200 mg (1.13 mmol) of 9-amino-2,3-dihydro-4,1-benzoxazepin-5(1H)-one in 20 mL of THF was added 280 mg (2 mmol) of 1,1′-carbonyldiimidazole and the reaction mixture was stirred overnight at room temperature. The reaction mixture was heated at 50° C. for 4 h and allowed to cool to room temperature. The reaction was concentrated in vacuo and the residue was dissolved in a mixture of ethyl acetate/n-hexane (1:1) and washed with water. The organics were dried over sodium sulfate, filtered, and concentrated in vacuo to give 286 mg (1.40 mmol, 70%) of the title compound.

1. temperatureThe reaction mixture was heated at 50° C. for 4 h
2. temperatureto cool to room temperature
3. concentrationThe reaction was concentrated in vacuo
4. dissolutionthe residue was dissolved in a mixture of ethyl acetate/n-hexane (1:1)
5. washwashed with water
6. dry with materialThe organics were dried over sodium sulfate
7. filtrationfiltered
8. concentrationconcentrated in vacuo