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AssigneeChengdu Easton Biopharmaceuticals Co., Ltd.
InventorsLeixin Wang, Huike Gu, Xiaochao Xian, Hong Chen, Ying Wang
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A hydrate of a VEGFR inhibitor, a crystal form thereof and a preparation method therefor are provided. The VEGFR inhibitor is 6-(6,7-dimethoxyquinazolin-4-yl-oxy)-N,2-dimethylbenzofuran-3-carboxamide, and the hydrate and the crystal form thereof have good physicochemical properties, and have good flowability, solubility, stability and bioavailability, and alleviated hygroscopicity. In addition, the preparation method is simple, has good repeatability, achieves high yield, and is easy to perform and environment-friendly, and the method requires only a small amount of solvents and facilitates recycling use, thus effectively reducing the cost on reagents, and enabling easy implementation of large-scale mass production.
A fruquintinib hydrate of formula (II):
A crystal form α of fruquintinib, wherein an X-ray powder diffraction pattern of the crystal form has characteristic peaks at 2θ angles of 7.2±0.2°, 8.6±0.2°, 14.4±0.2°, 15.2±0.2°, 20.4±0.2°, 22.3±0.2°, 24.0±0.2°, 26.1±0.2°, 26.4±0.2°, and 29.1±0.2°.
Dependencies are inferred from the claim text.