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Novel nitroimidazole drug as well as preparation method and application of novel nitroimidazole drug

A technology of nitroimidazoles and drugs, which is applied in the field of new nitroimidazoles and its preparation, and can solve problems such as unfavorable drug use, sheet bleeding, stomach discomfort, etc.

Active Publication Date: 2018-01-09
HC SYNTHETIC PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, nitroimidazole can cause genital erosion, flake hemorrhage, skin allergies, oral ulcers, nausea, stomach discomfort and other adverse reactions after oral administration, which can easily cause rejection in patients and is not conducive to medication.

Method used

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  • Novel nitroimidazole drug as well as preparation method and application of novel nitroimidazole drug
  • Novel nitroimidazole drug as well as preparation method and application of novel nitroimidazole drug
  • Novel nitroimidazole drug as well as preparation method and application of novel nitroimidazole drug

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Embodiment 1: Preparation of 2-trifluoromethylimidazole

[0035] Take 50ml of ammonia water and add it to a three-necked bottle, stir at room temperature, then take 10ml of trifluoroacetaldehyde hydrate and 10ml of glyoxal, mix them, and slowly add them dropwise to the ammonia water, react at room temperature for 2 hours, and add 20ml of ethyl acetate after the reaction is over. After two extractions for 30 min, the ethyl acetate layer was separated and dried with anhydrous magnesium sulfate, and the solvent was evaporated under reduced pressure at 60°C to obtain 8.9 g of a brown oily substance, namely 2-trifluoromethylimidazole.

Embodiment 2

[0036] Embodiment 2: Preparation of 2-methylimidazole

[0037] Take 50ml of ammonia water and add it to a three-necked bottle, stir at room temperature, then mix 10ml of acetaldehyde and 10ml of glyoxal, slowly add it dropwise to ammonia water, react at room temperature for 2 hours, after the reaction, add 20ml of ethyl acetate x 2 extractions for 30min , the ethyl acetate layer was separated and dried with anhydrous magnesium sulfate, and the solvent was distilled off under reduced pressure at 60°C to obtain 7.2 g of a brown solid, namely 2-methylimidazole.

Embodiment 3

[0038] Example 3: Preparation of 2-trifluoromethyl-5-nitroimidazole

[0039] Take 20ml of concentrated sulfuric acid and 5g of sodium sulfate into a three-necked flask, stir at room temperature, slowly add 5.0g of 2-trifluoromethylimidium, and start to heat up. After the temperature of the reaction solution reaches 150°C, slowly add 5ml of concentrated nitric acid dropwise, drop After the addition is complete, keep the reaction for 2 hours. After the reaction, cool down to 80°C and add 5ml of water, adjust the pH to 3-4 with ammonia water, a large amount of solids precipitate, filter, and dry at 60°C to obtain 2-trifluoromethyl-5-nitrate Kiimidazole 4.1g.

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PUM

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Abstract

The invention relates to a novel nitroimidazole compound as well as a preparation method and application of the novel nitroimidazole compound to medical science and specifically relates to a nitroimidazole compound as shown in a general formula (I), a preparation method of the nitroimidazole compound and a pharmaceutical composition containing the compound. The invention aims at synthesizing a novel compound of a series of nitroimidazole derivatives by modifying the structure of a nitroimidazole compound, the compound can be used for obviously reducing adverse reaction in clinic, meanwhile, the compound has a relatively ideal effect on protecting the liver and kidneys, and the clinical application of the compound is apparent.

Description

technical field [0001] The invention belongs to the technical field of medicinal chemistry, and in particular relates to a novel nitroimidazole drug and a preparation method and application thereof. Background technique [0002] At present, among the infectious diseases, the most common type is bacterial infection. If there is a lack of timely and effective treatment, it can lead to high mortality in severe cases. For example, foodborne diseases caused by Campylobacter, Salmonella, Escherichia coli O157 and Listeria monocytogenes bring huge economic losses and life threats to human beings every year. [0003] Antibiotics are considered to be the most beneficial weapon in the treatment of bacterial infectious diseases. However, with the increasing abuse of antibiotics, the problem of bacterial drug resistance is increasing. The speed of new antibiotic development is far lower than the speed of drug-resistant bacteria. Studies have shown that 25% of Streptococcus pneumoniae i...

Claims

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Application Information

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IPC IPC(8): C07D417/06C07D413/06C07F9/6558A61K31/5377A61K31/541A61K31/675A61P31/04A61P33/02
CPCY02A50/30
Inventor 张起愿刘晓鹏
Owner HC SYNTHETIC PHARMA CO LTD
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