反应详情

To a solution of 2-fluoro-5-(3-fluorophenyl)-N-(3-methoxyphenyl)benzamide (605 mg, 1.80 mmol, 1.0 eq) in THF (3 mL) was added dropwise a solution of BH3 (1 M in THF, 5.3 mL, 5.3 mmol, 2.9 eq) at 0° C. The reaction was heated at reflux overnight, then cooled to room temperature and quenched by addition of methanol and water. The reaction was diluted with EtOAc and water and the aqueous layer extracted further with EtOAc. The combined organic extracts were washed with brine, dried (Na2SO4), filtered and evaporated in vacuo. The crude residue was purified by flash chromatography (petroleum ether: EtOAc, 10:1) to give the title compound as a colourless oil (512 mg, 88%).

1. temperatureThe reaction was heated
2. temperatureat reflux overnight
3. customquenched by addition of methanol and water
4. additionThe reaction was diluted with EtOAc and water
5. extractionthe aqueous layer extracted further with EtOAc
6. washThe combined organic extracts were washed with brine
7. dry with materialdried (Na2SO4)
8. filtrationfiltered
9. customevaporated in vacuo
10. customThe crude residue was purified by flash chromatography (petroleum ether: EtOAc, 10:1)