Salt of aromatic heterocyclic derivative and application thereof
A technology for drugs and compounds, applied in the field of medicine, can solve problems such as research on compound salts or their crystal forms, and achieve the effects of good water solubility, good pharmacokinetic properties, and good biological activity.
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Embodiment 1
[0091] Embodiment 1 Maleate salt crystal form B of the present invention
[0092] 1. Preparation of maleate salt form B
[0093] Take the compound (0.5g) shown in formula (I) in a round bottom flask, add dichloromethane (8mL), dissolve at room temperature, add maleic acid (0.149g) (compound shown in formula (I) and maleic acid The molar ratio of the acid is 1 / 1.2), there is no obvious phenomenon, a large amount of white solids are precipitated after 1h, suspended for 12h, filtered and dried to obtain the maleate crystal form B product.
[0094] 2. Identification of maleate crystal form B
[0095] Identified by Empyrean X-ray powder diffraction (XRPD) analysis: using Cu-Kα radiation, with the following characteristic peaks expressed in angle 2θ: 8.88°±0.2°, 13.37°±0.2°, 15.40°±0.2°, 16.38°±0.2 °,16.83°±0.2°,17.94°±0.2°,20.17°±0.2°,20.80°±0.2°,20.99°±0.2°,22.14°±0.2°,22.95°±0.2°,24.49°±0.2°, 25.62°±0.2°, 27.00°±0.2°, 29.49°±0.2°, 29.98°±0.2°, 34.17°±0.2°, 37.22°±0.2°. The XR...
Embodiment 2
[0096] Embodiment 2 Citrate crystal form B of the present invention
[0097] 1. Preparation of citrate crystal form B
[0098] Get compound (0.5g) shown in formula (I) in round bottom flask, add dichloromethane (10mL), dissolve at room temperature clear, add citric acid (0.249g) (compound shown in formula (I) and citric acid The molar ratio was 1 / 1.2), without obvious phenomenon, a large amount of white solids were precipitated after 1h, suspended for 12h, filtered and dried to obtain citrate crystal form B.
[0099] 2. Identification of citrate crystal form B
[0100] (1) Analysis and identification by Empyrean X-ray powder diffraction (XRPD): using Cu-Kα radiation, with the following characteristic peaks expressed in angle 2θ: 5.66°±0.2°, 6.84°±0.2°, 7.72°±0.2°, 9.54 °±0.2°,11.31°±0.2°,13.69°±0.2°,16.22°±0.2°,17.00°±0.2°,19.17°±0.2°,20.56°±0.2°,22.99°±0.2°,23.92°± 0.2°, 25.86°±0.2°, 28.21°±0.2°, 30.05°±0.2°, 32.61°±0.2°, 34.43°±0.2°, 36.48°±0.2°, 37.63°±0.2°. The XRPD pa...
Embodiment 3
[0102] Embodiment 3 Sulfate crystal form A of the present invention
[0103] 1. Preparation of sulfate crystal form A
[0104] Take the compound (2g) shown in formula (I) in a round bottom flask, add ethyl acetate (10mL), warm up to 50 ° C to dissolve, then add sulfuric acid (0.6g) dropwise (dissolved in 2mL ethyl acetate, formula ( 1) The molar ratio of the compound shown in 1) to sulfuric acid is 1 / 1.2), and a white solid is separated out immediately, and after being suspended for 12 hours, it is filtered and dried to obtain about 2.3g of sulfate crystal form A product in total.
[0105] 2. Identification of sulfate crystal form A
[0106] Identified by Empyrean X-ray powder diffraction (XRPD) analysis: using Cu-Kα radiation, with the following characteristic peaks expressed in angle 2θ: 9.76°±0.2°, 14.55°±0.2°, 15.65°±0.2°, 16.35°±0.2 °,17.95°±0.2°,18.93°±0.2°,19.37°±0.2°,19.64°±0.2°,20.22°±0.2°,20.98°±0.2°,21.38°±0.2°,21.81°±0.2°, 22.18°±0.2°, 23.22°±0.2°, 23.60°±0.2°, ...
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