反应详情

温度

150 °C

(S)-tert-butyl (1-(3,6-dibromopyridin-2-yl)-2-(3,5-difluorophenyl)ethyl)carbamate (150 mg, 0.3 mmol), 3-methylazetidin-3-ol hydrochloride (75 mg, 0.6 mmol) was combined with cesium carbonate (397 mg, 1.2 mmol), palladium diacetate (10 mg, 0.015 mmol) and 2,2′-bis-(diphenylphosphino)-1,1′-binaphthyl (19 mg, 0.03 mmol) in 2 mL of toluene. The system was degassed and purged with argon and heated to 150° C. heating bath for 1 hour, the reaction mixture was cooled and diluted with ethyl acetate. The organic layer was washed with water and brine, and then dried over sodium sulfate. The crude was purified by flash chromatography eluting with EtOAc/hexanes to provided the title compound. MS (m/z) 499.72 [M+H]+.

1. customThe system was degassed
2. custompurged with argon
3. temperatureheating bath for 1 hour
4. temperaturethe reaction mixture was cooled
5. additiondiluted with ethyl acetate
6. washThe organic layer was washed with water and brine
7. dry with materialdried over sodium sulfate
8. customThe crude was purified by flash chromatography
9. washeluting with EtOAc/hexanes