Patent ID: 9120782
Filing Date: 2015-09-01
Classification: C07D

Abstract:
1. A crystallization method for preparing a crystal form of iloperidone, comprising the following steps: a) crude iloperidone is dissolved under stirring at 70° C.˜80° C. in an appropriate amount of ethyl acetate as a crystallization solvent and then filtered while hot to remove insoluble impurities in the solution to obtain a clear iloperidone solution; b) the resulting iloperidone solution is slowly cooled to 40° C.˜60° C.; c) 1% to 5% of iloperidone crystal seed relative to the weight of the crude iloperidone is slowly added thereto; d) stirring speed is controlled at 60 r/min-120 r/min, and stirring is performed for 1 hour to 3 hours at a constant temperature; e) the resulting solution is slowly cooled to room temperature under stirring, and then continuously stirred for 3 hours to 7 hours; f) the resulting crystalline slurry is filtered, and the resulting crystals are washed with ethyl acetate and dried to obtain iloperidone crystals, wherein the crystal form of iloperidone has the following X-ray diffraction pattern measured by copper cathode X-ray diffractometer and expressed as the interplanar spacing d, Bragg angle 2θ, intensity and relative intensity, wherein the relative intensity is expressed as a percentage relative to the strongest ray: