反应详情

温度

110 °C

A mixture of 3,5-dibromo-1-methyl-pyridin-2-one (2.000 mmol; 533.8 mg), tert-butyl N-[(3S)-3-piperidyl]carbamate (2.00 mmol; 401 mg), cesium carbonate (4.0 mmol; 1303 mg), Xantphos (0.3400 mmol; 202.8 mg), and tris(dibenzylideneacetone)dipalladium(0) (0.2000 mmol; 185.0 mg) in 1,4-Dioxane (10 mL) was purged with Argon, then sealed and stirred at 110° C. overnight. The mixture was cooled to room temperature and filtered through Celite. The filtrate was concentrated and the residue was purified on silica eluted with 0 to 100% EtOAc in Heptane to afford tert-butyl N-[(3S)-1-(5-bromo-1-methyl-2-oxo-3-pyridyl)-3-piperidyl]carbamate as a yellow solid (458.6 mg, 59%).

1. customwas purged with Argon
2. customsealed
3. temperatureThe mixture was cooled to room temperature
4. filtrationfiltered through Celite
5. concentrationThe filtrate was concentrated
6. customthe residue was purified on silica
7. washeluted with 0 to 100% EtOAc in Heptane