Crystal form of vortioxetine hydrochloride and preparation method thereof

A technology of vortioxetine and crystal form, applied in the field of drug crystals, can solve the problems of strong corrosiveness, toxicity and intractability of hydrobromic acid, and achieve the effects of relatively low toxicity and safe application

Active Publication Date: 2018-01-09
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Vortioxetine hydrobromide is currently used clinically, and hydrobromide has disadvantages due to the hydrobromic acid used in its production process, that is, hydrobromic acid is highly corrosive and toxic and difficult to handle industrially

Method used

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

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0101] Example 1: Preparation of vortioxetine hydrochloride crystal form II

[0102] Take 5g (16.7mmol) of vortioxetine, add 150ml of ethanol, stir and reflux, heat up to 40°C to dissolve, and slowly add 1.65g of concentrated hydrochloric acid (concentration: 37% by weight, 16.7mmol) dropwise to the vortioxetine under stirring conditions. In the ethanol solution of vortioxetine, solids precipitated during the dropping process, stirred for 20 minutes, cooled to room temperature naturally, after stirring for 1 hour, suction filtered, placed in a vacuum drying oven (40-50°C) to dry to obtain vortioxetine Hydrochloride salt form II.

Embodiment 2

[0103] Example 2: Preparation of vortioxetine hydrochloride crystal form II

[0104] Take 5g (16.7mmol) vortioxetine, add 50ml of acetone, stir and reflux, heat up to 70°C to dissolve, and slowly add 1.65g concentrated hydrochloric acid (concentration: 37% by weight, 16.7mmol) dropwise to vortioxetine under stirring condition. In the acetone solution of oxetine, solids precipitated during the dropwise addition, stirred for 20 minutes, cooled down to room temperature naturally, after stirring for 1 hour, suction filtered, and dried in a vacuum oven (40-50°C) to obtain vortioxetine Tine hydrochloride crystal form II.

Embodiment 3

[0105] Example 3: Preparation of Vortioxetine Hydrochloride Form II

[0106] Get 10g (33.5mmol) vortioxetine, add 50ml ethyl acetate, stir and reflux, heat up to 50°C to dissolve, under stirring, slowly add 3.3g concentrated hydrochloric acid (concentration is 37% by weight, 33.5mmol) dropwise to In the acetone solution of vortioxetine, solids precipitated during the dropwise addition, stirred for 20 min, cooled to room temperature, stirred for 0.5 h, filtered with suction, and dried in a vacuum oven (40-50°C) to obtain vortioxetine Tioxetine hydrochloride crystal form II.

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Abstract

The invention discloses a vortioxetine hydrochloride crystal substance and a preparation method thereof, including three new crystal forms of vortioxetine hydrochloride and preparation methods thereof and application to preparation of medicines for treating diseases such as depression. In addition to that the three new crystal forms of vortioxetine hydrochloride disclosed by the invention inherit characteristics of treating depression and the like of original vortioxetine medicines, the aspects such as dissolubility, safety and purity are improved, and the preparation of medicine preparations and the improvement of quality are facilitated.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical crystals, in particular, relates to the antidepressant vortioxetine hydrochloride and crystals or crystal forms thereof, especially vortioxetine hydrochloride and three crystal forms thereof, and also relates to the The preparation method of the salt and its crystal or crystal form and its use in the preparation of medicines for treating depression and other diseases. Background technique [0002] 1-[2-(2,4-Dimethylphenylsulfanyl)phenyl]piperazine, also known as Vortioxetine, which inhibits serotonin reuptake and has 5-HT1A Receptor agonists, 5-HT 1B receptor partial agonists and 5-HT 3, 5-HT1D and 5-HT 7 receptor antagonists; the diversity of the drug's action makes it neurological in several systems Transmission produces a regulatory effect, mainly regulating serotonin, and it is speculated that it can also regulate norepinephrine, dopamine, histamine, acetylcholine, GABA and glutamate s...

Claims

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Application Information

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Patent Type & AuthorityPatents(China)
IPC IPC(8): C07D295/096
CPCC07B2200/13C07D295/096
Inventor胡秀荣周新波顾建明汤谷平
OwnerZHEJIANG UNIV