反应详情

Dissolve [4-(2-azepan-1-yl-ethoxy)-phenyl]-[2-(2,5-difluoro-phenyl)-6-methoxy-naphthalen-1-yl]-methanone (1.74 g, 3.37 mmol) in 20 mL methylene chloride and chill in ice. Add to this solution 2.0 mL of boron tribromide (5.3 g, 21.2 mmol) and allow to come to room temperature. Pour into a two phase solution of saturated sodium bicarbonate and 3/1 chloroform/isopropanol. Separate the organic layer, wash with water and dry over 3 Å sieves. Evaporate the solvent and purify on a silica gel column eluting with a 0-10% methanol/methylene chloride gradient. Evaporate the solvent to yield 780 mg (46%) of the title compound.

1. temperaturechill in ice
2. customto come to room temperature
3. customSeparate the organic layer
4. washwash with water
5. customdry over 3 Å sieves
6. customEvaporate the solvent
7. custompurify on a silica gel column
8. washeluting with a 0-10% methanol/methylene chloride gradient
9. customEvaporate the solvent