Preparation method of ozagrel impurity

A technology of impurity and mass ratio, applied in the field of preparation of ozagrel impurities, can solve the problems of appearance variation, activity reduction, low drug content and the like

Inactive Publication Date: 2020-03-06
深圳振强生物技术有限公司
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Problems solved by technology

[0003] The impurities contained in the drug are the main factors affecting the purity of the drug. If the drug contains impurities exceeding the limit, it may change the physical and chemical constants, change the appearance, and affect the stability of the drug.
The increase of impurities will inevitably reduce the content of the drug or reduce the activity, and the toxic and side effects will increase significantly.

Method used

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  • Preparation method of ozagrel impurity
  • Preparation method of ozagrel impurity

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Embodiment Construction

[0020] Further description will be made below in conjunction with the accompanying drawings and specific embodiments.

[0021] Such as figure 1 and figure 2 As shown, the present invention provides a kind of preparation method of ozagrel impurity, comprises the following steps:

[0022] S1: adding methyl 4-bromomethyl cinnamate and sodium methoxide in a mass ratio of 5:1 to an appropriate amount of methanol to prepare a solution;

[0023] S2: stirring at room temperature for 2-16 hours to fully react the mixture in the solution to obtain a mixed solution containing ozagrel impurities;

[0024] S3: Concentrating the ozagrel impurity by vacuum rotary evaporation;

[0025] S4: Purify the ozagrel impurity by column chromatography.

[0026] For making 4-bromomethyl cinnamic acid methyl ester dissolve completely, the content of methyl alcohol is as many as possible, present embodiment adds 1 part of 4-bromomethyl cinnamic acid methyl ester and 0.2 part of sodium methylate in 10...

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Abstract

The invention relates to a preparation method of a zagrel impurity. The method includes the steps of: adding methyl 4-bromomethylcinnamate and sodium methoxide into a proper amount of methanol according to a mass ratio of 5:1, and blending the substances into a dilute solution; performing stirring for 2-16h under a room temperature condition to enable full reaction of the mixture, thus obtaining amixed solution containing ozagrel impurity; concentrating the ozagrel impurity by vacuum rotary evaporation method; and carrying out purification treatment on the ozagrel impurity by column chromatography process. The method provided by the invention can simply and directly acquire an ozagrel impurity reference substance, also provides convenience for impurity analysis and research of ozagrel crude drugs and preparations thereof, and provides a detection method and judgment basis for production and medication safety of ozagrel.

Description

technical field [0001] The present invention relates to the technical field of drug impurity inspection and preparation, in particular to a method for preparing ozagrel impurities. Background technique [0002] Sodium ozagrel, chemical name (E)-3-[4-(1H-imidazol-1-methyl)yl]-2-sodium acrylate (1), is the first thromboxane synthase ( TX) inhibitors were put on the market under the trade name Cataclot by Japan Ono Pharmaceutical Co., Ltd. in 1989. Sodium ozagrel can hinder the production of thromboxane (TXA2) by the prostate (PGH2), and promote the conversion of PGH2 derived from platelets into endothelial cells, which are used to synthesize PGI2, thereby improving the abnormal balance between TXA2 and prostaglandin PGI2, and achieving the effect of inhibiting platelets. Aggregates and dilates blood vessels. Clinically, ozagrel sodium is mainly used for the treatment of acute thrombotic cerebral infarction and the movement disorder associated with cerebral infarction. [00...

Claims

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Application Information

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IPC IPC(8): C07C67/31C07C67/48C07C67/56C07C69/734
CPCC07C67/31C07C67/48C07C67/56C07C69/734
Inventor 李少龙
Owner 深圳振强生物技术有限公司
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