反应详情

To a stirred solution of ethyl 2-[2,4-difluoro-3-[[2-fluoro-5-(3-fluorophenyl)phenyl]methylamino]phenoxy]acetate (II(a)) (290 mg, 0.7 mmol, 1.0 eq) in MeOH (30 mL) was added K2CO3 (28 mg, 0.2 mmol 0.3 eq). The reaction was heated at reflux overnight. The solvent was removed in vacuo and the residue obtained was diluted with water and neutralized by addition of 1M HCl. The aqueous layer was further extracted with EtOAc and the combined organic extracts were washed with brine, dried (Na2SO4), filtered and evaporated in vacuo. The residue was purified by chromatography (EtOAc:petroleum ether, 0:1 to 1:20) to give the title compound an oil (130 mg, 46%).

1. temperatureThe reaction was heated
2. temperatureat reflux overnight
3. customThe solvent was removed in vacuo
4. customthe residue obtained
5. extractionThe aqueous layer was further extracted with EtOAc
6. washthe combined organic extracts were washed with brine
7. dry with materialdried (Na2SO4)
8. filtrationfiltered
9. customevaporated in vacuo
10. customThe residue was purified by chromatography (EtOAc:petroleum ether, 0:1 to 1:20)