反应详情

To 8-bromo-2-(2,2-dimethyl-1,3-dioxolan-4-yl)quinoline (101 mg, 0.328 mmol) in toluene (1.3 mL) was added tert-butyl piperidin-4-ylmethylcarbamate (84.3 mg, 0.393 mmol), Pd(OAc)2 (7.3 mg, 0.033 mmol), Binap-rac (25 mg, 0.039 mmol) and Cs2CO3 (235 mg, 0.721 mmol). The reaction was purged twice with nitrogen and heated at reflux overnight. The reaction mixture was cooled to ambient temperature and filtered through Celite, and the solids were washed with EtOAc (20 mL). The filtrate was concentrated, and the crude material was purified by silica gel chromatography (EtOAc/Hexane 1:6) provided final product.

1. customThe reaction was purged twice with nitrogen
2. temperatureheated
3. temperatureat reflux overnight
4. filtrationfiltered through Celite
5. washthe solids were washed with EtOAc (20 mL)
6. concentrationThe filtrate was concentrated
7. customthe crude material was purified by silica gel chromatography (EtOAc/Hexane 1:6)