3-(1-Piperazinyl)-1,2-benzisothiazole → Ziprasidone

Participants

Reaction Conditions

Reaction Steps

To de-ionized water (2.0 Lit), was added 5-(2-chloroethyl)-6-chloro-oxindole (100 g) and 1-(1,2-benzisothiazol-3-yl)piperazine (210 g) at 30-35° C. The mixture was slowly heated under stirring to 98-100° C. over 60-80 minutes. The resultant mass was stirred for 10-15 hours at 98-100° C. After completion of reaction as monitored by HPLC, the suspended solid material was filtered at 98-100° C. The wet cake so obtained was suspended in de-ionized water (2.0 Lit) and heated to 90-95° C. and maintained at this temperature for 30 minutes. The solid suspension was filtered at 90-95° C. The wet cake was further added to isopropyl alcohol (1.5 Lit) and stirred for 2 hours at 30-35° C. The solids were filtered and washed with isopropyl alcohol (500 ml) and dried under vacuum at 50-55° C. for 7-8 hours till moisture content was not more than 1.0% w/w.

Provenance & Evidence