反应详情

温度

120 °C

To a mixture of 3-bromo-7-methoxyquinoline (Intermediate 13, 380 mg, 1.6 mmol), 4-boronobenzoic acid (266 mg, 1.6 mmol) and Na2CO3 (848 mg, 8.0 mmol) in DME/H2O/EtOH (5 mL, V/V/V=1/1/0.5) was added Pd(dppf)Cl2 (585 mg, 0.8 mmol). The mixture was heated to 120° C. by microwave for 1 h. The mixture was partitioned between water (20 mL) and ethyl acetate (20 mL). The aqueous phase was separated and acidified to pH=3 with 1 N HCl. The precipitate was filtered and dried in vacuo to afford product as a powder (130 mg, 29.1%).

1. customThe mixture was partitioned between water (20 mL) and ethyl acetate (20 mL)
2. customThe aqueous phase was separated
3. filtrationThe precipitate was filtered
4. customdried in vacuo