Anti-infective drug and preparation method and application thereof

An anti-infection and drug technology, applied in the field of medicine, can solve the problems of drug toxicity and side effects

Pending Publication Date: 2020-09-01
HC SYNTHETIC PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] But there are also more and more common drug-resistant bacteria and toxic side effects of drugs

Method used

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  • Anti-infective drug and preparation method and application thereof
  • Anti-infective drug and preparation method and application thereof
  • Anti-infective drug and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0079] Example 1: Preparation of 2-methyl-5-nitro-1-(((S)-oxiran-2-yl)methyl)1H-imidazole

[0080]

[0081] Weigh 100g of left-ornidazole and add it into 500ml of dichloromethane, stir and dissolve, cool down to -10~-15℃; weigh 36.5g of sodium hydroxide, add 500ml of water, stir and dissolve, let cool, slowly add dropwise into dichloromethane, Control the temperature not to exceed -10°C. After the addition, keep it warm at 0-5°C for 2 hours, separate the dichloromethane layer, extract the water layer with 100ml of dichloromethane, combine the dichloromethane layers, and add 100ml of water to the dichloromethane layer for washing. Twice, add an appropriate amount of anhydrous sodium sulfate to dry, filter, and concentrate the filtrate under reduced pressure to obtain 75.7 g of a brown oil.

Embodiment 2

[0082] Example 2: Preparation of 2-methyl-5-nitro-1-(((R)-oxiran-2-yl)methyl)1H-imidazole

[0083]

[0084] Weigh 100g of dex-ornidazole and add it into 500ml of dichloromethane, stir and dissolve, cool down to -10~-15°C; weigh 36.5g of sodium hydroxide, add 500ml of water, stir and dissolve, let it cool, and slowly add it dropwise into dichloromethane, Control the temperature not to exceed -10°C. After the addition, keep it warm at 0-5°C for 2 hours, separate the dichloromethane layer, extract the water layer with 100ml of dichloromethane, combine the dichloromethane layers, and add 100ml of water to the dichloromethane layer for washing. Twice, add an appropriate amount of anhydrous sodium sulfate to dry, filter, and concentrate the filtrate under reduced pressure to obtain 72.5 g of a brown oil.

Embodiment 3

[0085] Example 3: Preparation of 2-methyl-5-nitro-1-((oxiran-2-yl)methyl)1H-imidazole

[0086]

[0087] Weigh 100g of ornidazole and add it into 500ml of dichloromethane, stir and dissolve, cool down to -10~-15℃; weigh 36.5g of sodium hydroxide, add 500ml of water, stir and dissolve, let cool, slowly add dropwise into dichloromethane, control The temperature should not exceed -10°C. After the addition, keep it warm at 0-5°C for 2 hours, separate the dichloromethane layer, extract the water layer with 100ml of dichloromethane, combine the dichloromethane layers, and add 100ml of water to the dichloromethane layer to wash for 2 hours. Once, add an appropriate amount of anhydrous sodium sulfate to dry, filter, and concentrate the filtrate under reduced pressure to obtain 76.3 g of a brown oil.

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Abstract

The invention provides an anti-infective drug, the structure of which is shown as a formula I. The anti-infective drug provided by the invention comprises a stereoisomer, a hydrate, a deuterated substance, an ester, a solvate, a crystal form, a metabolite, and a pharmaceutically acceptable salt or a prodrug, and has stronger bacterial activity and a wider antibacterial spectrum so as to treat infectious diseases.

Description

technical field [0001] The invention relates to an anti-infection drug and its preparation method and application, belonging to the technical field of medicine. Background technique [0002] Antibiotics are currently the first choice for humans to treat bacterial infectious diseases, but the excessive use and abuse of antibiotics has made the problem of bacterial drug resistance increasingly serious. The rapid development of drug-resistant bacteria of various antibiotics and antibacterial drugs has seriously threatened the lives and health of patients with infectious diseases. Exploring new anti-drug-resistant drugs has become a research hotspot in the medical field at home and abroad. Quinolones antibacterial drugs target bacterial deoxyribonucleic acid (DNA), hinder DNA gyrase, further cause irreversible damage to bacterial DNA, and achieve antibacterial effects. It has bactericidal effect on a variety of Gram-negative bacteria, and is widely used in the treatment of geni...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4709A61K31/497A61K31/675A61K31/4375A61K31/542A61K31/5365A61P31/00A61P31/02A61P31/04
CPCA61K31/4709A61K31/497A61K31/675A61K31/4375A61K31/542A61K31/5365A61P31/00A61P31/02A61P31/04
Inventor 杨成张起愿
Owner HC SYNTHETIC PHARMA CO LTD
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