反応 #2298667

反応方程式

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

K2CO3

3--chloropropoxybenzene

acetonitrile

→

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

収率 47.0%

溶媒

water

反応条件

後処理

1. 1
   温度at reflux under nitrogen for 30 hours
2. 2
   抽出the aqueous mixture was extracted with ethyl acetate
3. 3
   抽出The ethyl acetate extract
4. 4
   洗浄was washed with brine
5. 5
   乾燥dried with MgSO4
6. 6
   濃縮concentrated
7. 7
   その他to afford 6.2 g of a damp,
8. 8
   その他The compound was recrystalized twice from ethanol

実験手順

A mixture of 6-fluoro-3-(4-piperidinyl)-1,2-benzisoxazole (4.0 g, 0.0182 mol), K2CO3 (3.0 g, 0.0218 mol), KI (100 mg), 3--chloropropoxybenzene (3,4 g, 0.0200 mol), 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, being solid. The compound was recrystalized 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.

出典