Reacción #41845

Ecuación de reacción

sulfolane

3-piperazinylbenzo[d]isothiazole

6-chloro-5-(2-chloroethyl)indolin-2-one

potassium carbonate

→

5-(2-(4-(1,2-benzisothiazol-3-yl)-1-piperazinyl)ethyl)-6-chloro-1,3-dihydro-2H-indol-2-one

Rendimiento 74.8%

Disolventes

water

Condiciones de reacción

Tratamiento posterior

1. 1
   OtroIn glass-lined reactor placed
2. 2
   TemperaturaThe contents of the flask were initially heated to 75° C. to 80° C. for 2 hrs
3. 3
   TemperaturaThen temperature was raised to 95° C. to 100° C.
4. 4
   workup.ADDITIONwas added to the reaction mixture
5. 5
   workup.STIRRINGstirred
6. 6
   FiltraciónThe product was filtered off
7. 7
   Lavadowashed with water
8. 8
   Otrodried

Procedimiento

In glass-lined reactor placed 21.1 Kg (96.34 mole) of 3-piperazinylbenzo[d]isothiazole; 31 kg (134.7 moles) of 6-chloro-5-(2-chloroethyl)indolin-2-one; 1.1 kg of potassium iodide; 20.0 kg (111.92 mole) of potassium carbonate and 63.2 lit of sulfolane. The contents of the flask were initially heated to 75° C. to 80° C. for 2 hrs. Then temperature was raised to 95° C. to 100° C. and stirred till completion of the reaction. After completion of the reaction 210 lit of DM water was added to the reaction mixture and stirred. The product was filtered off and washed with water and dried to obtain 29.75 kg of 5-(2-(4-(1,2-benzisothiazol-3-yl)-1-piperazinyl)ethyl)-6-chloro-1,3-dihydro-2H-indol-2-one (Ziprasidone).

Fuente