Novel polymorph of pazopanib hydrochloride and preparation process thereof
AssigneeFormosa Laboratories, Inc.
InventorSheng-Kai KO
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Abstract
The present disclosure provides a crystalline form F of Pazopanib HCl, which is characterized by an X-ray diffraction (XRD) pattern having peaks at about 11.3, 14.6, 16.9, 19.5, 19.7, 23.5 and 25.9°±0.2° 2θ. The present disclosure also provides a preparation process of a crystalline form F of Pazopanib HCl.
Claims20
A crystalline form F of Pazopanib HCl, characterized by an X-ray diffraction (XRD) pattern having peaks at about 11.3, 14.6, 16.9, 19.5, 19.7, 23.5 and 25.9°±0.2° 2θ.
A preparation process of a crystalline form F of Pazopanib HCl, comprising following steps:
- (a) mixing N-(2-chloropyrimidin-4-yl)-N,2,3-trimethyl-2H-indazol-6-amine (CPMI) and 5-amino-2-methylbenzenesulfonamide (AMBS) in a solvent to obtain a mixture, wherein the solvent comprises MeOH;
- (b) heating the mixture to react the CPMI with the AMBS;
- (c) distilling a portion of the solvent, and cooling the mixture to a temperature ranged from 0° C. to 20° C.;
- and
- (d) isolating solids from the mixture and drying the solids to give a crystalline form F of Pazopanib HCl.
A preparation process of a crystalline form F of Pazopanib HCl, comprising following steps:
- (A) adding Pazopanib HCl with a crystalline form A into a solvent to obtain a mixture, wherein the solvent comprises MeOH;
- (B) stirring the mixture at room temperature for 48 hr or more;
- and
- (C) isolating solids from the mixture and drying the solids to give a crystalline form F of Pazopanib HCl.
Dependencies are inferred from the claim text.