反应详情

Intermediate B (4.04 g) and 4-formylphenylboronic acid (1.56 g) were suspended in 150 mL of acetonitrile and treated with 150 mL of 1 M sodium carbonate solution. To this was added dichloro-bis-(triphenylphosphine)-palladium(II) (608 mg) and the mixture was heated at reflux for 2.5 hours. The reaction mixture was filtered and the residue washed with EtOAc, the filtrates were combined and washed with water, and brine, dried over MgSO4, and concentrated. MPLC silica gel chromatography eluting with 0-30% EtOAc in hexane, produced 3.77 g of the title compound (M+H 492).

1. temperaturethe mixture was heated
2. temperatureat reflux for 2.5 hours
3. filtrationThe reaction mixture was filtered
4. washthe residue washed with EtOAc
5. washwashed with water, and brine
6. dry with materialdried over MgSO4
7. concentrationconcentrated
8. washMPLC silica gel chromatography eluting with 0-30% EtOAc in hexane