反应详情

5-Chloro-2-fluorophenylboronic acid (2.7 g, 15.48 mmol), 2-chloropyridin-4-amine (1.531 g, 11.91 mmol), sodium carbonate (5.96 ml, 11.91 mmol), and bis(triphenylphosphine) palladium chloride (0.836 g, 1.191 mmol) were combined in dioxane (54 mL) and refluxed for 3 hours. The reaction was cooled, the solvent removed in vacuo and the reaction mixture partitioned between brine and EtOAc. The organic layer was separated, dried over MgSO4 filtered and purified using NH silica column chromatography and a gradient of 5-95% EtOAc in hexanes to afford the title compound as a white solid (522 mg; 20%). ESI-MS: m/z 223.1 (M+H).

1. temperaturerefluxed for 3 hours
2. temperatureThe reaction was cooled
3. customthe solvent removed in vacuo
4. customthe reaction mixture partitioned between brine and EtOAc
5. customThe organic layer was separated
6. dry with materialdried over MgSO4
7. filtrationfiltered
8. custompurified