Crystal forms of vortioxetine organic acid salt and preparation method thereof
A technology of vortioxetine and crystal form, applied in organic chemistry, nervous system diseases, drug combination, etc., can solve the problems of strong corrosion, toxicity, and difficult handling of hydrobromic acid, and achieve improved water solubility and bioavailability Improve and enhance the effect of the application range
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[0101] Example 1: Preparation of Vortioxetine Paraben Hydrate
[0102] Add 2.9g vortioxetine to 15ml acetone:water (1:1) mixed solvent, heat to 60°C, add 1.4g p-hydroxybenzoic acid, stir and dissolve, continue stirring for 2 hours, and then naturally cool down to At 30°C, a white solid was precipitated, filtered with suction, and dried in a vacuum drying oven (40-50°C) to obtain vortioxetine p-hydroxybenzoate hydrate.
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[0103] Example 2: Preparation of Vortioxetine Paraben Hydrate
[0104] Add 15g of vortioxetine to 150ml of ethyl acetate, heat to 50°C to dissolve, dissolve 7.0g of p-hydroxybenzoic acid in 10ml of hot water and add dropwise to the vortioxetine solution, stir for 1 hour, and naturally cool down to At 20°C, white crystals were slowly precipitated. After 48 hours, suction filtration was performed to obtain a white solid, which was dried in a vacuum drying oven (40-50°C) to obtain vortioxetine p-hydroxybenzoate hydrate.
Example Embodiment
[0105] Example 3: Preparation of Vortioxetine Paraben Hydrate
[0106] Dissolve 2.9g of vortioxetine in 120ml of 10% ethanol aqueous solution, add 1.4g of p-hydroxybenzoic acid, heat to 70°C, continue stirring for 2h, after dissolving, take it to an ice-water bath at 0°C for crystallization, and slowly precipitate white crystals , 24 hours later, suction filtration to obtain a white solid, which is dried in a vacuum drying oven (40-50° C.) to obtain vortioxetine p-hydroxybenzoate hydrate.
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