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A kind of medicine for treating pneumonia and preparation method thereof

A technology of pneumonia and drugs, applied in the field of medicine, to achieve excellent results, strong antibacterial activity, and short routes

Active Publication Date: 2020-05-12
MUDANJIANG MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] However, the use of a large number of antibiotics has led to the emergence of a large number of drug-resistant bacteria, such as drug-resistant Streptococcus pneumoniae, methicillin-resistant Staphylococcus aureus, etc., which has become the most difficult problem in the current clinical anti-infection treatment

Method used

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  • A kind of medicine for treating pneumonia and preparation method thereof
  • A kind of medicine for treating pneumonia and preparation method thereof
  • A kind of medicine for treating pneumonia and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

preparation example 1

[0037] Preparation 1: 7-(4-fluorobenzyloxy)-4,5-dihydrotetrazole[1,5-a]quinoline (Compound 1)

[0038]

[0039] Step 1: Add 3,4-dihydroquinolin-2(1H)-one (5.0mmol) and triphenylphosphine (20.0mmol), diethyl azodicarboxylate (20.0mmol) to THF (30mL) 1-butyl-3-methyl-imidazolium hexafluorophosphoric acid (2 mL) was added, and then diphenylphosphoryl azide (20.0 mmol) was added, and the mixture was stirred at 40° C. for 15 hours, and the progress of the reaction was monitored by TLC. After the reaction was complete, the reaction solution was cooled to room temperature and diluted with water (50mL), then extracted with ethyl acetate (80mL×3) and the combined extracts were washed with saturated aqueous sodium bicarbonate solution, and the organic layer was washed with anhydrous sulfuric acid Sodium dried and concentrated. The residue was purified by flash chromatography on a silica gel column, using petroleum ether:dichloromethane (v:v=10:1) as the eluting solvent to obtain 4,5...

preparation example 2

[0047] Preparation 2: 7-(4-Chlorobenzyloxy)-4,5-dihydrotetrazole[1,5-a]quinoline (Compound 2)

[0048]

[0049] Step 1 and Step 2 are the same as Preparation Example 1.

[0050] Step 3: Mix 7-bromo-4,5-dihydrotetrazolo[1,5-a]quinoline (2.0mmol), (4-chloro-phenyl)-methanol (2.2mmol), palladium acetate (0.2 mmol), cesium carbonate (4.0 mmol) and 2-dicyclohexylphosphine-2,4,6-triisopropylbiphenyl (0.4 mmol) were added to toluene (30 mL), and stirred for 5 minutes under nitrogen protection. Then it was heated to 85° C. under sealed condition and reacted for 5 hours. After filtration and concentration under reduced pressure, the residue was purified by flash chromatography on a silica gel column, using cyclohexane:ethyl acetate (v:v=7:1) as the eluting solvent, and the main fractions were collected and evaporated to dryness under reduced pressure, and then weighed with ethanol Crystallization gave 0.52 g of the target product.

[0051] Melting point: 188-190°C;

[0052] MS m...

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Abstract

The invention relates to a tetrazoloquinoline compound capable of being used for treating pneumonia. The tetrazoloquinoline compound has stronger antibacterial activity against various bacteria such as streptococcus pneumoniae and staphylococcus aureus, and has antibacterial activity significantly superior to known drugs especially for drug-fast streptococcus pneumoniae and drug-fast staphylococcus aureus. In addition, the preparation method is short in route, few in steps and high in total product yield, and is suitable for industrial large-scale production.

Description

technical field [0001] The invention relates to the field of medicine, in particular, the invention relates to a medicine for treating pneumonia, and also relates to a preparation method of the medicine. Background technique [0002] Pneumonia refers to the infection of the lung parenchyma in the terminal airways, alveoli, and interstitial tissues of the lungs. The main clinical symptoms are fever, cough, expectoration, and blood in the sputum, which may be accompanied by chest pain or dyspnea, etc., and there are abnormal chest X-rays. Change. Severely ill patients may involve the circulatory, digestive and nervous systems and appear corresponding clinical symptoms. Pneumonia can be caused by disease microorganisms such as bacteria, viruses, mycoplasma, chlamydia, fungi, etc., physical and chemical factors, immune damage, allergies, and drugs. The most common pneumonia is bacterial pneumonia. [0003] The treatment of pneumonia caused by bacteria, mycoplasma, chlamydia, a...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D471/04A61P31/04A61P11/00A61K31/437
CPCA61P11/00A61P31/04C07D471/04
Inventor 袁玫倪薪吕玉凤姜爱英朱仁英
Owner MUDANJIANG MEDICAL UNIV