Novel crystal form of Vortioxetine hydrobromate and preparation method for novel crystal form of Vortioxetine hydrobromate

A technology of vortioxetine hydrobromide and cetine hydrobromide compound, which is applied in the field of new crystal form of vortioxetine hydrobromide and its preparation, can solve problems such as inability to achieve simple and stable operation Good performance, to meet the effect of large-scale industrial production

Inactive Publication Date: 2016-07-27
SHANGHAI AOBO PHARMTECH INC LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] Patent WO2010094285 discloses an isopropanol solvate of vortioxetine hydrobromide, which is used to remove impurities. The solvate itself cannot be used as an API for pharmaceutical use

Method used

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  • Novel crystal form of Vortioxetine hydrobromate and preparation method for novel crystal form of Vortioxetine hydrobromate
  • Novel crystal form of Vortioxetine hydrobromate and preparation method for novel crystal form of Vortioxetine hydrobromate
  • Novel crystal form of Vortioxetine hydrobromate and preparation method for novel crystal form of Vortioxetine hydrobromate

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] At room temperature, weigh 1 g of vortioxetine hydrobromide, add it into 6 ml of N,N-dimethylformamide, raise the temperature to 75° C. to dissolve it completely, and filter it. The filtrate was added to 50ml of water cooled to 2°C, a solid was precipitated, and the stirring was continued for 10 minutes, followed by suction filtration, and drying to obtain off-white new crystal form δ of vortioxetine hydrobromide.

Embodiment 2

[0036] At room temperature, weigh 1 g of vortioxetine hydrobromide, add it into 6 ml of N,N-dimethylformamide, raise the temperature to 75° C. to dissolve it completely, and filter it. The filtrate was added to 50ml of water cooled to 5°C, and a solid was precipitated, and the stirring was continued for 20 minutes, followed by suction filtration, and drying to obtain off-white new crystal form δ of vortioxetine hydrobromide.

Embodiment 3

[0038] At room temperature, weigh 100g of vortioxetine hydrobromide, add it into 600ml of N,N-dimethylformamide, raise the temperature to 75°C to completely dissolve it, and filter. The filtrate was added to 5 L of water cooled to 2.5°C, and a solid was precipitated, and the stirring was continued for 2 hours, followed by suction filtration, and drying to obtain off-white vortioxetine hydrobromide new crystal form δ.

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Abstract

The invention relates to a novel crystal form of Vortioxetine hydrobromate and a preparation method for the novel crystal form of the Vortioxetine hydrobromate. The novel crystal form of the Vortioxetine hydrobromate is named a crystal form sigma, wherein in an X-ray powder diffraction atlas using Cu-K alpha radiation detection, the crystal form sigma has characteristic peaks when a 2[theta] angle is about 4.0 degrees, 11.5 degrees, 15.5 degrees, 17.7 degrees, 19.1 degrees, 20.8 degrees, 22.9 degrees, 27.2 degrees or 28.6 degrees. The invention also provides a method for preparing the novel crystal form sigma of the Vortioxetine hydrobromate. The method is simple and convenient and is good in reproducibility, and the obtained novel crystal form sigma of the Vortioxetine hydrobromate is high in purity and good in stability, so that the method is applicable to industrial production.

Description

technical field [0001] The invention relates to a new crystal form of vortioxetine (1-[2-(2,4-methylphenylthio)phenyl]piperazine) hydrobromide and a preparation method thereof. technical background [0002] The chemical name of vortioxetine is 1-[2-(2,4-methylphenylsulfanyl)phenyl]piperazine, and its structural formula is shown in formula I below: [0003] [0004] Vortioxetine was jointly developed by Denmark's Lundbeck Pharmaceuticals and Japan's Takeda Pharmaceuticals, and was approved by the FDA in September 2013 for the treatment of major depressive disorder (MDD) in adults. In October of the same year, the Human Medicines Committee (CHMP) under the European Medicines Agency (EMA) recommended that Vortioxetine be used for the treatment of major depression and issue a European marketing authorization. [0005] Vortioxetine is a selective serotonin reuptake inhibitor, 5-HT 3A Receptor Inhibitors, 5-HT 7 Receptor Inhibitors and Partial 5-HT 1B Compared with the exis...

Claims

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Application Information

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IPC IPC(8): C07D295/096
Inventor 顾虹任国宾
Owner SHANGHAI AOBO PHARMTECH INC LTD
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