反应详情

温度

75 °C

A mixture of (S)-tert-butyl 2-((S)-1-amino-1-oxo-3-(4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl)propan-2-ylcarbamoyl)piperidine-1-carboxylate (92 mg), 2-(4-bromo-2-(methylsulfonyl)phenyl)acetonitrile (75 mg), bis(1,2-bis(diphenylphosphino)ethane)-palladium(0) (8.29 mg, 9.17 μmol) and 2 N aqueous potassium carbonate (0.229 mL) in dioxane (3 mL) was heated at 75° C. for 14 h. The mixture was poured onto an Isolute HM-N cartridge, eluting with DCM, collecting about 100 mL of eluent. The eluent was concentrated in vacuo to leave a brown oil. The residue was purified by flash silica chromatography, eluting with ethyl acetate to give the subtitle compound as a white solid (80 mg).

1. additionThe mixture was poured onto an Isolute HM-N cartridge
2. washeluting with DCM
3. customcollecting about 100 mL of eluent
4. concentrationThe eluent was concentrated in vacuo
5. customto leave a brown oil
6. customThe residue was purified by flash silica chromatography
7. washeluting with ethyl acetate