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Rivaroxaban acetic acid solvate and preparation method thereof
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A technology for rivaroxaban and solvate, applied in the field of rivaroxaban acetic acid solvate and its preparation, can solve the problems of not providing comparative data, not providing solubility test and the like, so as to improve bioavailability, increase Clinical efficacy and good stability
Active Publication Date: 2020-08-11
LUNAN PHARMA GROUP CORPORATION
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Problems solved by technology
Rivaroxaban has polymorphic forms, and WO2007 / 039132 discloses crystal form characterization data and preparation methods of crystal form I, crystal form II, crystal form III, amorphous, hydrate, NMP and THF solvent compounds; EP2573084A1 reports The B1, B2 and E crystal forms of rivaroxaban and the method of mutual conversion between them; CN02292332A and CN104211693B respectively reported the new APO-A crystal form and IV crystal form of rivaroxaban, compared with other crystal forms , with better thermal stability and higher solubility, but did not provide comparative data; CN102056923B reported rivaroxaban malonate co-crystal and its preparation method, and its solubility is said to be more than 2.5 times that of rivaroxaban , but also did not provide solubility test and specific data support
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Embodiment 1
[0047] Embodiment 1 Preparation of rivaroxaban acetic acid solvate
[0048] Add 1 g of crystal form I rivaroxaban into 100 mL of acetic acid, heat to 60°C, stir for 2 hours, rivaroxaban is completely dissolved, then add 10 mL of ethanol, slowly cool down to 10°C, filter the clear solution to remove insoluble particles, The filtrate was placed in a beaker, sealed with a parafilm, punctured, volatilized naturally at room temperature, crystallized for 4 days, filtered, and dried under reduced pressure at 50°C to obtain rivaroxaban acetic acid solvate. Yield: 98.0%, HPLC purity: 99.96%.
Embodiment 2
[0049] Embodiment 2 Preparation of rivaroxaban acetic acid solvate
[0050] Add 1 g of Form I rivaroxaban to 200 mL of acetic acid, heat to 50 ° C, stir for 0.5 h, rivaroxaban is completely dissolved, then add 50 mL of ethanol, slowly cool down to 0 ° C, filter the clear solution to remove insoluble particles , the filtrate was placed in a beaker, sealed with a parafilm, punctured, naturally volatilized at room temperature, crystallized for 3 days, filtered, and dried under reduced pressure at 50°C to obtain rivaroxaban acetic acid solvate. Yield: 97.3%, HPLC purity: 99.95%.
Embodiment 3
[0051] Embodiment 3 Preparation of rivaroxaban acetic acid solvate
[0052] Add 1 g of Form I rivaroxaban to 45.5 mL of acetic acid, heat to 85°C, stir for 3 hours, rivaroxaban is completely dissolved, then add 2.3 mL of ethanol, slowly cool down to 25°C, filter the clear solution to remove insoluble The particles and the filtrate were placed in a beaker, sealed with a parafilm, pierced, volatilized naturally at room temperature, crystallized for 5 days, filtered, and dried under reduced pressure at 50°C to obtain rivaroxaban acetic acid solvate. Yield: 96.7%, HPLC purity: 99.93%.
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Abstract
The invention belongs to the technical field of crystal form drug molecules, and particularly relates to a rivaroxabanacetic acid solvate and a preparation method thereof. According to the rivaroxabanacetic acid solvate, Cu-Kalpha radiation is used for radiation and an X-raydiffraction spectrum expressed by 2theta has diffraction peaks at 3.48 + / -0.2 degrees, 7.00 + / -0.2 degrees, 14.10 + / -0.2 degrees, 17.67 + / -0.2 degrees, 21.27 + / -0.2 degrees, 28.62 + / -0.2 degrees and 39.69 + / -0.2 degrees; the preparation method of the rivaroxabanacetic acid solvate is simple, efficient and suitable for industrial production, the prepared crystal form substance is high in purity and good in stability, and the solubility reaches 67.5 mg / L.
Description
technical field [0001] The invention belongs to the technical field of crystaldrug molecules, and in particular relates to rivaroxaban acetic acid solvate and a preparation method thereof. Background technique [0002] Rivaroxaban (Rivaroxaban), the chemical name is 5-chloro-nitrogen-({(5S)-2-oxo-3-[-4-(3-oxo-4-morpholinyl)phenyl]-1, 3-oxazolidin-5-yl}methyl)-2-thiophene-carboxamide is a low-molecular-weight, highly selective oral inhibitor of blood coagulation factor Xa jointly developed by Bayer and Johnson & Johnson for 10 years, which can be used for Prevention, secondary prevention and / or treatment of different thromboembolic diseases, especially prevention and treatment of reocclusion and restenosis after myocardial infarction, angina (including unstable angina), angioplasty or aortocoronary bypass , stroke, transient ischemic attack, and peripheral arterial occlusive disease. Since it was first launched in Canada in September 2008, it has been approved in more than...
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