Hydrochloric Acid → Lurasidone hydrochloride

Participants

Reaction Conditions

Reaction Steps

100 g lurasidone free base of Formula (H) and 3500 mL methanol were added to round bottom flask at 25° C. to 35° C. and heated to 60 to 65° C. for 10 min. To the reaction mass 14% 74.5 g isopropanolic hydrochloric acid was added and stirred for 1 hour at same temperature. The reaction mixture was charcoalized and filtered. The filtrate was distilled to remove methanol under vacuum below 45° C. The residue was again treated with 500 mL methanol at 45° C. and stirred for 30 min. The reaction mixture was cooled to 25° C. The reaction mixture was further cooled to 0 to 5° C. and stirred for 2 hours. The precipitated product was filtered and washed with 100 mL methanol to afford crystalline lurasidone hydrochloride of Formula (1). X-ray powder diffraction pattern (FIG. 1), DSC (FIG. 2).

Provenance & Evidence