반응 #41845

반응 방정식

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

수율 74.8%

용매

water

반응 조건

후처리

1. 1
   기타In glass-lined reactor placed
2. 2
   온도The contents of the flask were initially heated to 75° C. to 80° C. for 2 hrs
3. 3
   온도Then temperature was raised to 95° C. to 100° C.
4. 4
   workup.ADDITIONwas added to the reaction mixture
5. 5
   workup.STIRRINGstirred
6. 6
   여과The product was filtered off
7. 7
   세척washed with water
8. 8
   기타dried

실험 절차

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).

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