Novel method for preparation of vortioxetine hydrobromide crystal form alpha

A technology of vortioxetine hydrobromide and crystal form, which is applied in the fields of pharmacy and chemical industry, and the new preparation field of vortioxetine hydrobromide crystal form α, which can solve the problem of low sample purity and unsatisfactory performance. To the problems of pharmaceutical grade requirements and complex operation, it can achieve the effects of good preparation processability, excellent stability, and excellent preparation dissolution rate.

Active Publication Date: 2017-05-10
JIANGSU HANSOH PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This method has disadvantages such as poor reproducibility, complex operation, low sample purity, and failure to meet the requirements of pharmaceutical grades.

Method used

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  • Novel method for preparation of vortioxetine hydrobromide crystal form alpha
  • Novel method for preparation of vortioxetine hydrobromide crystal form alpha
  • Novel method for preparation of vortioxetine hydrobromide crystal form alpha

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Dissolve 1 g of vortioxetine hydrobromide in 10 ml of N,N-dimethylformamide to form a solution, and add the resulting solution dropwise to 100 ml of methyl tert-butyl ether at a temperature of 20°C, stirring After 10 minutes, it was filtered and dried to obtain 0.78g of crystal form α, which was detected by X-ray diffraction, and the results were as follows: figure 1 As shown, it is basically consistent with the XRD spectrum of crystal form α reported in patent CN101472906B.

Embodiment 2

[0023] Dissolve 1 g of vortioxetine hydrobromide in 10 ml of N,N-dimethylacetamide, heat to 40°C to form a solution, and add the resulting solution dropwise to 150 ml of methyl tert-butyl In base ether, after stirring for 10 minutes, filter and dry to obtain 0.82g crystal form α, and its XRD pattern is consistent with figure 1 Basically the same.

Embodiment 3

[0025] Dissolve 2 g of vortioxetine hydrobromide in 10 ml of chloroform to form a solution. Add the resulting solution dropwise to 100 ml of isopropyl ether at a temperature of -15° C., keep stirring for 10 minutes, filter and dry to obtain 1.60 g crystal form α, its XRD pattern and figure 1 Basically the same.

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Abstract

The invention relates to a novel method for preparation of a vortioxetine hydrobromide crystal form alpha. The method includes steps: dissolving vortioxetine hydrobromide into a good solvent, dropwise adding to a poor solvent at a low temperature, and crystallizing to obtain the crystal form alpha. The novel method has advantages of high yield, high purity, low energy consumption, simplicity in operation, safety, environment friendliness, high repeatability and the like and is especially suitable for large-scale chemical production in the pharmaceutical and chemical industry.

Description

technical field [0001] The invention belongs to the technical field of crystal forms, and in particular relates to a new preparation method of vortioxetine hydrobromide crystal form α, and the application of the preparation method in the fields of pharmacy and chemical industry. Background technique [0002] Vortioxetine is a new type of antidepressant drug developed by Lundbeck of Denmark and Takeda Pharmaceutical of Japan. Its chemical name is 1-[2-(2,4-dimethylbenzene Sulfuryl) phenyl] piperazine, the structural formula is as follows: [0003] [0004] On September 30, 2013, the U.S. Food and Drug Administration (FDA) approved vortioxetine hydrobromide (trade name Brintellix) for the treatment of adult patients with major depressive disorder. The approval of the drug is based on a comprehensive clinical development project. Efficacy and safety data for the treatment of major depressive disorder, the project consists of 7 pivotal studies, including 6 short-term studies...

Claims

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Application Information

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IPC IPC(8): C07D295/096
CPCC07B2200/13C07D295/096
Inventor 何雷余俊杨宝海
Owner JIANGSU HANSOH PHARMA CO LTD
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