反应详情

To a solution of N-[[2-fluoro-5-(3-fluorophenyl)phenyl]methyl]-3-methoxy-aniline (512 mg, 1.60 mmol, 1.0 eq) in CH2Cl2 (10 mL) at −70° C. was added BBr3 (0.6 mL, 65.3 mmol, 40.8 eq). The reaction was warmed to room temperature and stirred for 1 h. The reaction was then cooled to 0° C. and quenched by addition of water. The pH of the solution was adjusted to pH 7 with aqueous Na2CO3, then extracted with EtOAc. The organic extract was washed with water and brine, dried (Na2SO4), filtered and evaporated in vacuo to give the title compound as a colourless oil (460 mg, 94%).

1. temperatureThe reaction was then cooled to 0° C.
2. customquenched by addition of water
3. extractionextracted with EtOAc
4. extractionThe organic extract
5. washwas washed with water and brine
6. dry with materialdried (Na2SO4)
7. filtrationfiltered
8. customevaporated in vacuo