Water → Iloperidone

Participants

Reaction Conditions

Reaction Steps

6-Fluoro-3-(4-piperidinyl)-1,2benzisoxazole hydrochloride (IV) (25.5 gr., 0.1 mol.), potassium carbonate (27.0 gr., 0.2 mol.) and 80 ml. of N,N-dimethyl formamide (DMF) were charged into a clean and dry 500 ml 4 neck R.B.Flask. 4-(3′-chloropropoxy)-3-methoxybenzonitrile (V) (20.0 gr., 0.08 mol.) and potassium iodide (680 mg.) were added at about 30° C. The resultant reaction mixture was heated to about 90° C. and stirred for about 9 hrs. After completion of the reaction, the reaction mixture was cooled to about 30° C. and 400 ml. of water were charged. After stirring for 30 min., the separated solid was filtered and the solid obtained and washed with 50 ml. of water. Recrystallized from methanol and water (3:1) using decolourising carbon to afford the title compound as an off-white crystalline powder. Yield: 28.4 gr (% Yield: 78%).

Provenance & Evidence