反应详情

温度

120 °C

To a solution of 0.19 mmol (5-Iodo-1,3-dihydro-isoindol-2-yl)-[5-methanesulfonyl-2-((S)-2,2,2-trifluoro-1-methyl-ethoxy)-phenyl]-methanone (Example C3) in 1 ml DMF under argon was added successively 0.018 mmol tetrakistriphenylphosphine, 0.28 mmol phenyl boronic acid and 0.56 mmol potassium carbonate. The reaction mixture was heated at 120° C. for 2 hours then cooled to room temperature and filtered. The filtrate was evaporated to dryness and the residue was treated with sat. NaCl. The resulting mixture was extracted 3 times with dichloromethane. The organics phases were dried over sodium sulfate and evaporated. The crude compound was purified on a 10 g of Si-Amine cartridge: n-Heptane/Ethylacetate to provide the title compound (50%). Off-white solid. MS (m/e): 490.0 [M+H]+, 100%).

1. temperaturethen cooled to room temperature
2. filtrationfiltered
3. customThe filtrate was evaporated to dryness
4. additionthe residue was treated with sat. NaCl
5. extractionThe resulting mixture was extracted 3 times with dichloromethane
6. dry with materialThe organics phases were dried over sodium sulfate
7. customevaporated
8. customThe crude compound was purified on a 10 g of Si-Amine cartridge