Reaktion #83863

Reaktionsgleichung

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

K2CO3

3-chloropropoxybenzene

acetonitrile

→

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

Ausbeute 47.0%

Lösungsmittel

water

Reaktionsbedingungen

Aufarbeitung

1. 1
   Temperaturat reflux under nitrogen for 30 hours
2. 2
   Extraktionthe aqueous mixture was extracted with ethyl acetate
3. 3
   ExtraktionThe ethyl acetate extract
4. 4
   Waschenwas washed with brine
5. 5
   Trocknendried with MgSO4
6. 6
   Einengenconcentrated
7. 7
   Sonstigeto afford 6.2 g of a damp, beige solid
8. 8
   SonstigeThe compound was recrystallized twice from ethanol

Vorschrift

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.

Quelle