反应详情

温度

0 °C

Dissolve [2-(2,4-difluoro-phenyl)-6-methoxynaphthalen-1-yl]-[4-(2-piperidin-1-yl-ethoxy)-phenyl]-methanone (10.8 g, 21.5 mmol) in methylene chloride (200 mL). Add 2M HCl in ether (21.5 mL, 43 mmol) and concentrate in vacuo. Redissolve the foam in methylene chloride (200 mL) and cool to 0° C. under nitrogen. Slowly add boron tribromide (10.1 mL, 107 mmol) and stir at 0° C. for 30 minutes. Slowly pour into saturated aqueous sodium bicarbonate and extract with 20% WA in chloroform. Dry the organic layer with sodium sulfate, filter and concentrate in vacuo to yield 10.5 g (100%) of the title compound.

1. concentrationconcentrate in vacuo
2. dissolutionRedissolve the foam in methylene chloride (200 mL)
3. extractionextract with 20%
4. dry with materialDry the organic layer with sodium sulfate
5. filtrationfilter
6. concentrationconcentrate in vacuo