反应详情

To a solution of isopropyl 2-[3-[(3-bromo-5-methyl-phenyl)methylamino]-2,4-difluoro-phenoxy]acetate (176 mg, 0.4 mmol, 1.0 eq) in acetonitrile (15 mL) was added 3-fluorophenylboronic acid (86 mg, 0.61 mmol, 1.5 eq), K2CO3 (142 mg, 1.03 mmol, 2.5 eq) and Pd(dppf)Cl2 (15 mg, 0.02 mmol, 0.05 eq). The mixture was heated at reflux overnight then the solvent was removed in vacuo. The residue was diluted with CH2Cl2, washed with water, dried (MgSO4), filtered and evaporated in vacuo. The residue was purified by chromatography (petroleum ether: EtOAc, 150:1 to 60:1) to give the title compound as an oil (140 mg, 77%).

1. temperatureThe mixture was heated
2. temperatureat reflux overnight
3. customthe solvent was removed in vacuo
4. additionThe residue was diluted with CH2Cl2
5. washwashed with water
6. dry with materialdried (MgSO4)
7. filtrationfiltered
8. customevaporated in vacuo
9. customThe residue was purified by chromatography (petroleum ether: EtOAc, 150:1 to 60:1)