反应详情

(N4-CBz-cytosin-1-yl)acetic acid (2.42 g, 8 mmol) was azeotroped with benzene (3×25 mL) and dried under vacuum. 32 mL of anhydrous DMF was added under N2 followed by the addition of DIC (1.57 mL, 8 mmol). The reaction was stirred at room temperature for 2-3 minutes, then treated with piperazinone (8.8 mmol, 881.1 mg), and the reaction mixture was left to stir for 48 hours. The reaction mixture was concentrated by rotary evaporation, washed successively with 0.1 N citric acid solution (2×10 mL) and water (2×15 mL), and then dried in a dessicator, affording N-[(N4-CBz-cytosin-1-yl)acetyl]-piperazinone as a white solid.

1. customdried under vacuum
2. addition32 mL of anhydrous DMF was added under N2
3. waitthe reaction mixture was left
4. stirringto stir for 48 hours
5. concentrationThe reaction mixture was concentrated by rotary evaporation
6. washwashed successively with 0.1 N citric acid solution (2×10 mL) and water (2×15 mL)
7. customdried in a dessicator