Hydrochloric Acid → Paliperidone

Participants

Reaction Conditions

Reaction Steps

A mixture of dilute hydrochloric acid and paliperidone palmitate heated to 75-80° C. and the reaction was maintained for 2 hours at 75-80° C., monitored the reaction by HPLC for absence of paliperidone palmitate and cooled the reaction mass to 25-30° C. The reaction mass was washed with methylene chloride, added a mixture of methylene chloride and methanol to aqueous layer, cooled the contents to 10° C., adjusted pH 10-12 with 20% sodium hydroxide in water solution at 10-30° C., extracted the compound into methylene chloride at basic condition and washed the methylene chloride layer with purified water and the separated methylene chloride layer treated with activated carbon, filtered the carbon through hyflow bed, washed with methylene chloride, the methylene chloride was distilled off completely under vacuum and added Isopropyl alcohol, heated the contents to reflux temperature and slowly cooled to 25-30° C., stirred for 1 hour at the same temperature, filtered the isolated compound, washed the wet compound with Isopropyl alcohol and dried under vacuum at 55-60° C. to get pure paliperidone.

Provenance & Evidence