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Edaravone compound with stable crystal form

A compound and crystal form technology, applied in the field of edaravone compounds, can solve the problems of insoluble edaravone and the like, and achieve the effects of simple and easy method, good stability and improved yield

Inactive Publication Date: 2012-02-15
TIANJIN SONGRUI MEDICAL TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0015] The object of the present invention is to provide a kind of Edaravone compound of stable crystal form, it can overcome the deficiencies in the prior art, effectively solve the problems such as Edaravone is difficult to dissolve in water

Method used

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  • Edaravone compound with stable crystal form
  • Edaravone compound with stable crystal form
  • Edaravone compound with stable crystal form

Examples

Experimental program
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Effect test

Embodiment 1

[0032] 1) Put 5.0 g of crude Edaravone into a single-mouth bottle, add 80 ml of pure ethanol aqueous solution (ethanol: pure water = 1:3), and stir to dissolve at 45°C;

[0033] 2) Then adjust the pH of the Edaravone solution to 4.0 with hydrochloric acid at room temperature, add 600ml of diethyl ether and acetone mixture (diethyl ether: acetone = 1:2.5), and stir and crystallize at 20°C for 3 hours;

[0034] 3) The precipitated Edaravone crystals were collected by filtration, washed with 100ml of the above ether and acetone mixture and dried in an oven at 30°C to obtain 4.5g of Edaravone crystals with a yield of 90% and a purity of 99.7%.

Embodiment 2

[0036] 1) Put 5.0 g of crude Edaravone into a single-mouth bottle, add 100 ml of pure ethanol aqueous solution (ethanol: pure water = 1:3), and stir to dissolve at 48°C;

[0037] 2) Then adjust the pH of the Edaravone solution to 4.2 with hydrochloric acid at room temperature, add 500ml of isopropyl ether and acetone mixture (isopropyl ether: acetone = 1:3), stir and crystallize at 30°C for 5 hours;

[0038] 3) The precipitated Edaravone crystals were collected by filtration, washed with 100ml of the above isopropyl ether and acetone mixture and dried in an oven at 30°C to obtain 4.55g of Edaravone crystals with a yield of 91% and a purity of 99.6 %.

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Abstract

The invention belongs to the technical field of medicines and provides an edaravone compound with a stable crystal form and a preparation method thereof. The method comprises the following steps of: stirring to dissolve a crude edaravone product in a pure aqueous solution of ethanol, regulating the pH value to be 3 to 5 by using hydrochloric acid, adding a mixed solution in which the volume ratio of ethers to ketones is 1:(1-4), and stirring to precipitate crystals; and filtering, collecting, washing, and performing vacuum drying to obtain the edaravone compound. The yield is 90 percent, and the purity is 99.6 percent.

Description

technical field [0001] The invention relates to the field of medicine, in particular to an edaravone compound in a stable crystal form. Background technique [0002] Edaravone [0003] Chemical name: 3-Methyl-1-phenyl-2-pyrazolin-5-one (3-Methyl-1-phenyl-2-pyrazolin-5-one); [0004] Molecular formula: C 10 h 10 N 20 ; [0005] Molecular weight: 174.20; [0006] Structural formula: [0007] [0008] Since the main ring of Edaravone is a five-membered ring ketone, the carbonyl group is adjacent to N, and the N at position 2 is connected to an unsaturated bond, which is easy to oxidize, so the molecular structure is very unstable, and it will be oxidized to There is no active substance, and it is easy to produce high molecular impurities, which will cause harm to the human body. In addition, because there are no hydrophilic groups such as hydroxyl and carboxyl in the structure, and methyl and phenyl are insoluble in water, the long-term dissolution process will aggra...

Claims

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Application Information

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IPC IPC(8): C07D231/26
Inventor 张昊
Owner TIANJIN SONGRUI MEDICAL TECH
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