A kind of tinidazole process impurity and synthetic method thereof

A technology of process impurities and synthesis methods, applied in the directions of organic chemistry, instruments, measuring devices, etc., can solve the problems of affecting safety and effectiveness, reducing the quality of tinidazole preparations, reducing the purity and yield of tinidazole products, and the like, Achieve perfect quality standards, good application prospects and mild reaction conditions

Active Publication Date: 2022-05-31
河北广祥制药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] 2-Methyl-5-nitroimidazole is an important raw material for the synthesis of tinidazole, but 2-methyl-5-nitroimidazole also contains various impurities, and some impurities may participate in the synthesis of tinidazole In the synthesis reaction, if the content of impurities in the 2-methyl-5 nitroimidazole raw material is higher, the purity and yield of the tinidazole product will be directly reduced, which will lead to a reduction in the quality of the tinidazole preparation, and even affect the quality of the tinidazole preparation. Safety and efficacy of drugs in clinical use

Method used

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  • A kind of tinidazole process impurity and synthetic method thereof
  • A kind of tinidazole process impurity and synthetic method thereof
  • A kind of tinidazole process impurity and synthetic method thereof

Examples

Experimental program
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Embodiment 1

[0047]

[0048]

[0049] MS: [M+H]

Embodiment 2

[0054]

[0055]

[0056] MS: [M+H]

Embodiment 3

[0061]

[0062]

[0063] MS: [M+H]

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Abstract

The invention relates to the technical field of chemical synthesis, and specifically discloses a technical impurity of tinidazole and a synthesis method thereof. The structure of the tinidazole process impurity is shown in formula (I), and the synthetic method comprises the steps of: taking 4-nitroimidazole and hydroxyethyl sulfide as raw materials, taking benzene compounds as solvent, under the action of concentrated sulfuric acid Condensation reaction is carried out to obtain the compound shown in formula (II); under the catalysis of soluble molybdate, the compound shown in formula (II) is oxidized by hydrogen peroxide to obtain the tinidazole process impurity shown in formula (I). The present invention prepares tinidazole process impurities with a purity of more than 99.7% through a specific synthesis process, solves the problem of the source of tinidazole process impurities reference substances, and is conducive to further improving the production of tinidazole raw materials or preparations thereof Quality Standard.

Description

A kind of tinidazole technological impurity and its synthesis method technical field The present invention relates to chemical synthesis technical field, relate in particular to a kind of tinidazole process impurity and synthetic method thereof. Background technique Tinidazole belongs to nitroimidazole antibacterials, is a kind of medicine of efficient anti-amebic and anti-anaerobic bacteria, and the Compared with the traditional anti-anaerobic bacteria metronidazole, it has the advantages of better efficacy and less side effects. Tinidazole is often combined with other antianaerobic agents It is used in combination with various anaerobic bacteria to treat diseases such as sepsis, respiratory tract infection, abdominal cavity and pelvic infection caused by various anaerobic bacteria. should be less. 2-methyl-5-nitroimidazole is an important raw material for synthesizing tinidazole, but, also in 2-methyl-5-nitroimidazole Contains a variety of impurities, some impur...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D233/94G01N30/02G01N30/06G01N30/86
CPCC07D233/94G01N30/02G01N30/06G01N30/8679Y02A50/30
Inventor 孙立杰石红超田鹏美魏赛丽张伟丽延春霞张雪彤孙朝振
Owner 河北广祥制药有限公司
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