反应详情

To a solution of 4-bromo-6-cyanoindole (900 mg, 4.1 mmol) in dichloromethane (30 mL) was added 4-benzyloxy-3-fluorobenzeneboronic acid (2.0 g, 8.1 mmol), triethylamine (1.2 mL, 8.6 mmol), copper (II) acetate (1.5 g, 8.2 mmol) and powdered 4A molecular sieves (2.0 g). The reaction mixture was stirred at room temperature in the presence of air for 16 hours. Further quantities of 4-benzyloxy-3-fluorobenzeneboronic acid (500 mg), triethylamine (0.3 mL) and copper acetate (375 mg) were added and the mixture stirred at room temperature in the presence of air for a further 16 hours. The mixture was filtered and the solid washed with dichloromethane. The filtrate was concentrated at reduced pressure. The product was purified by silica gel chromatography eluting with 2-40% ethyl acetate in hexane to yield the title compound (D13), (1.09 g).

1. stirringthe mixture stirred at room temperature in the presence of air for a further 16 hours
2. filtrationThe mixture was filtered
3. washthe solid washed with dichloromethane
4. concentrationThe filtrate was concentrated at reduced pressure
5. customThe product was purified by silica gel chromatography
6. washeluting with 2-40% ethyl acetate in hexane