反应详情

To a stirred solution of 2,4-difluoro-3-[[5-(3-fluorophenyl)-2-methoxy-3-methyl-phenyl]methylamino]phenol (47 mg, 0.13 mmol, 1.0 eq) in acetone (5 mL) was added Cs2CO3 (61.5 mg, 0.19 mmol, 1.5 eq). The resulting mixture was stirred for 30 min at room temperature then ethyl bromoacetate (25.2 mg, 0.15 mmol, 1.2 eq) was added. The resulting mixture was stirred for 1 h then diluted with water and extracted with EtOAc. The combined organic extracts were washed with water and brine, dried (Na2SO4) and evaporated in vacuo. The residue was purified by column chromatography (petroleum ether:EtOAc, 1:0 to 20:1) to give the title compound as an oil (64 mg, 86%).

1. stirringThe resulting mixture was stirred for 1 h
2. extractionextracted with EtOAc
3. washThe combined organic extracts were washed with water and brine
4. dry with materialdried (Na2SO4)
5. customevaporated in vacuo
6. customThe residue was purified by column chromatography (petroleum ether:EtOAc, 1:0 to 20:1)