Réaction #41845

Équation de réaction

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

Rendement 74.8%

Solvants

water

Conditions de réaction

Traitement

1. 1
   AutreIn glass-lined reactor placed
2. 2
   TempératureThe contents of the flask were initially heated to 75° C. to 80° C. for 2 hrs
3. 3
   TempératureThen temperature was raised to 95° C. to 100° C.
4. 4
   workup.ADDITIONwas added to the reaction mixture
5. 5
   workup.STIRRINGstirred
6. 6
   FiltrationThe product was filtered off
7. 7
   Lavagewashed with water
8. 8
   Autredried

Mode opératoire

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).

Source