反应详情

温度

80 °C

Compound 11 (242 mg, 0.716 mmol), 1-(2-(4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenoxy)ethyl)pyrrolidine 25 [prepared by Specific Method A2] (500 mg, 1.58 mmol), K2CO3 (247 mg, 1.79 mmol), and Pd(dppf)2Cl2 (524 mg, 0.072 mmol) were combined in a pyrex tube. After purging with N2, DMF (7.3 mL) and H2O (1.45 mL) were added and the tube was sealed. The mixture was heated at 80° C. for 5 h. After cooling to RT, CH2Cl2 was added and the organic layers were washed with H2O, followed by brine. The organic layers were then dried over Na2SO4 and concentrated to a brown oil. Flash chromatography (SiO2, gradient eluent: 0-15% MeOH in CH2Cl2), followed by trituration with EtOAc and filtration afforded compound 26.

1. customAfter purging with N2, DMF (7.3 mL) and H2O (1.45 mL)
2. additionwere added
3. customthe tube was sealed
4. temperatureAfter cooling to RT
5. additionCH2Cl2 was added
6. washthe organic layers were washed with H2O
7. dry with materialThe organic layers were then dried over Na2SO4
8. concentrationconcentrated to a brown oil
9. filtrationFlash chromatography (SiO2, gradient eluent: 0-15% MeOH in CH2Cl2), followed by trituration with EtOAc and filtration