反应详情

Convert [2-(2,5-difluoro-phenyl)-6-methoxy-naphthalen-1-yl]-[4-(2-piperidin-1-yl-ethoxy)-phenyl]-methanone (1.8 g, 3.5 mmol) to the hydrochloride salt and dissolve it in 300 mL methylene chloride. Chill the mixture in ice and slowly add boron tribromide (5.0 mL, 53.0 mmol) with swirling. Allow the mixture to come to room temperature and stir for two hours. Add to this mixture acetonitrile (15 mL) slowly and with stirring which produces an orange precipitate. Pour the mixture into saturated sodium bicarbonate with stirring, separate the organic layer and dry with molecular sieves to give 1.5 g of the title compound (86%).

1. temperatureChill the mixture in ice
2. customto come to room temperature
3. stirringwith stirring which
4. customproduces an orange precipitate
5. stirringwith stirring
6. customseparate the organic layer
7. customdry with molecular sieves