反应详情

To a solution of 2,4-dichloro-3-[[2-fluoro-5-(3-fluorophenyl)phenyl]methylamino]phenol (150 mg, 0.4 mmol, 1.0 eq) in DMF (50 mL), was added K2CO3 (220 mg, 0.6 mmol, 1.5 eq) and the solution was stirred at room temperature for 30 min. BrCH2CO2Et (100 mg, 1.6 mmol, 4.0 eq) was added dropwise and the reaction was stirred overnight. The reaction was quenched by addition of water (200 mL) and extracted with EtOAc. The combined organic extracts were dried (Mg2SO4), filtered and evaporated under reduced pressure and the residue obtained purified by column chromatography (EtOAc:petroleum ether, 0:1 to 1:10) to give the title compound (130 mg, 70%).

1. stirringthe reaction was stirred overnight
2. customThe reaction was quenched by addition of water (200 mL)
3. extractionextracted with EtOAc
4. dry with materialThe combined organic extracts were dried (Mg2SO4)
5. filtrationfiltered
6. customevaporated under reduced pressure
7. customthe residue obtained
8. custompurified by column chromatography (EtOAc:petroleum ether, 0:1 to 1:10)