反应 #83863

反应方程式

6-fluoro-3-(4-piperidinyl)-1,2-benzisoxazole

K2CO3

3-chloropropoxybenzene

acetonitrile

→

6-fluoro-3-[1-(3-phenoxypropyl)-4-piperidinyl]-1,2-benzisoxazole

收率 47.0%

溶剂

water

反应条件

后处理

1. 1
   温度at reflux under nitrogen for 30 hours
2. 2
   萃取the aqueous mixture was extracted with ethyl acetate
3. 3
   萃取The ethyl acetate extract
4. 4
   洗涤was washed with brine
5. 5
   干燥dried with MgSO4
6. 6
   浓缩concentrated
7. 7
   其他to afford 6.2 g of a damp, beige solid
8. 8
   其他The compound was recrystallized twice from ethanol

实验过程

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.

来源