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Crystal form of vortioxetine hydrobromide and preparation method thereof

A technology for vortioxetine crystals and vortioxetine, which is applied in the field of medicine, can solve problems such as solvent residues and the like, and achieve the effects of complete crystallization, short preparation time and low usage of organic solvents

Inactive Publication Date: 2020-05-01
SHANDONG BESTCOMM PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The solvents used in refining vortioxetine hydrobromide are unconventional reagents, and there is a potential risk of solvent residue

Method used

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  • Crystal form of vortioxetine hydrobromide and preparation method thereof
  • Crystal form of vortioxetine hydrobromide and preparation method thereof
  • Crystal form of vortioxetine hydrobromide and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0053] Take 5 g of vortioxetine hydrobromide and 50 ml of sec-butanol, and add them to a 100 ml round bottom flask. Raise the temperature to 80°C, if it is not dissolved, add 5ml of water, dissolve it, and maintain it for 0.5h. The temperature was lowered, and a large amount of solids were precipitated at 15°C, and the temperature was continued to drop to 0°C. Insulate and grow the crystal for 2h. Suction filtration to obtain a white solid. It was air-dried at 90°C for 2 hours and weighed 4.33g. Yield 86.6%, purity 99.9%. Its XRPD pattern and figure 1 be consistent.

Embodiment 2

[0055] Take 5 g of vortioxetine hydrobromide and 50 ml of sec-butanol, and add them to a 100 ml round bottom flask. Raise the temperature to 81°C, if it is not dissolved, add 2.5ml of water, dissolve it, and maintain it for 0.5h. When the temperature was lowered to 45°C, a large amount of solids were precipitated, and the temperature was continued to drop to 0°C. Insulate and grow the crystal for 2h. Suction filtration to obtain a white solid. Air-dried at 90°C for 2 hours, weighing 4.73g. Yield 94.6%, purity 99.9%. Its XRPD pattern and figure 1 be consistent.

Embodiment 3

[0057] Take 5 g of vortioxetine hydrobromide and 50 ml of sec-butanol, and add them to a 100 ml round bottom flask. Raise the temperature to 82°C, if it is not dissolved, add 1.7ml of water, dissolve it, and maintain it for 0.5h. When the temperature was lowered to 47°C, a large amount of solids were precipitated, and the temperature was continued to drop to 0°C. Insulate and grow the crystal for 2h. Suction filtration to obtain a white solid. It was air-dried at 90°C for 2 hours and weighed 4.78g. Yield 95.6%, purity 99.9%. Its XRPD pattern and figure 1 be consistent.

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Abstract

The invention provides a crystal form of vortioxetine hydrobromide, and also relates to a preparation method for the crystal form. The crystal form of the vortioxetine hydrobromide provided by the invention has good physicochemical stability and purity, facilitates large-scale production, is simple to operate, and has wide application prospect.

Description

[0001] 1. Technical field [0002] The invention belongs to the technical field of medicine, in particular to a crystal form of vortioxetine hydrobromide, and also to a preparation method of the crystal form of vortioxetine hydrobromide. [0003] 2. Background technology [0004] Vortioxetine Hydrobromide (Vortioxetine Hydrobromide), the chemical name is 1-[2-(2,4-dimethylphenylsulfanyl)phenyl]piperazine hydrobromide, its structural formula is shown in the following formula I . On September 30, 2013, the U.S. Food and Drug Administration (FDA) approved vortioxetine hydrobromide for the treatment of adult patients with major depressive disorder, with a trade name of Brintellix. The approval is based on efficacy and safety data from a comprehensive clinical development program for the treatment of major depressive disorder. The program consists of 7 pivotal studies, including 6 short-term studies lasting 6-8 weeks, and 1 long-term study lasting 24-64 weeks. Statistically signi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D295/096
CPCC07B2200/13C07D295/096
Inventor 凌浩王振华
Owner SHANDONG BESTCOMM PHARMA CO LTD
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