反应详情

A mixture of 6-fluoro-3-(4-piperidinyl)-1,2-benzisoxazole (4.0 g, 18.2 mmol), K2CO3 (3.0 g, 21.8 mmol), KI (100 mg), 3-chloropropoxybenzene (3.4 g, 20.0 mmol), and acetonitrile was stirred at reflux under nitrogen for 30 hours. The reaction was poured into water and the aqueous mixture was extracted with ethyl acetate. The ethyl acetate extract was washed with brine, dried with MgSO4 and concentrated to afford 6.2 g of a damp, beige solid. The compound was recrystallized twice from ethanol to yield (47%) of 6-fluoro-3-[1-(3-phenoxypropyl)-4-piperidinyl]-1,2-benzisoxazole as a light beige solid, m.p.=78°-80° C.

1. temperatureat reflux under nitrogen for 30 hours
2. extractionthe aqueous mixture was extracted with ethyl acetate
3. extractionThe ethyl acetate extract
4. washwas washed with brine
5. dry with materialdried with MgSO4
6. concentrationconcentrated
7. customto afford 6.2 g of a damp, beige solid
8. customThe compound was recrystallized twice from ethanol