反应详情

To a solution of compound 8 (100 mg, 0.27 mmol) in CH3CN (5 mL) was added K2CO3 (74 mg, 0.54 mmol). After addition, the resulting mixture was stirred at room temperature for 10 min. Then 3-bromo-1,1,1-trifluoro-propane (47.8 mg, 0.27 mmol) in CH3CN (5 mL) was added dropwise via a syringe with stirring. The mixture was stirred at 60° C. overnight, and then the mixture was filtered off, the filtrate was concentrated to give compound 9 (97 mg, 80%) as a white solid, which was used for the next step directly without purification. LC-MS tR=1.392 min in 2 min chromatography, MS (ESI) m/z 467.2 [M+H]+.

1. additionAfter addition
2. stirringwith stirring
3. stirringThe mixture was stirred at 60° C. overnight
4. filtrationthe mixture was filtered off
5. concentrationthe filtrate was concentrated