Hydrochloric Acid → Ziprasidone Hydrochloride

Participants

Reaction Conditions

Reaction Steps

To substantially pure ziprasidone base (100 g), was added dichloromethane (2.0 Lit) and stirred for 15-20 minutes at 30-35° C. To this, was added ethereal solution of hydrogen chloride (95.7 ml) over a period of 5-10 min at 30-35° C. under stirring. The suspension was further stirred for 17-20 hours at 32-35° C. and separated solids were filtered under vacuum and nitrogen atmosphere at 32-35° C. The wet solid was washed with diethyl ether (100 ml) and was suspended in water (500 ml) at 20-25° C. It was stirred for 30 minutes at 20-25° C. The mass was filtered and re-suspended in water (500 ml) and after stirring for approximately 1 hour, the cake was filtered and washed with a pre-cooled mixture of water and isopropanol (2×250 ml, 1:0.25). The washings were found to be free of acidity (pH of about 7). The product obtained was dried under vacuum at 55-60° C. for 12-15 hours till the moisture content was less than 0.5% w/w.

Provenance & Evidence