A kind of indole drug molecule for medical care, sterilization and disinfection, its preparation method and application

A drug molecule, sterilization and disinfection technology, applied in the fields of botanical equipment and methods, applications, disinfectants, etc., can solve the problem of infiltration diagnosis and treatment technology that cannot be guaranteed

Active Publication Date: 2021-12-24
THE FIRST AFFILIATED HOSPITAL OF HENAN UNIV OF SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The cleaning, disinfection and sterilization of medical instruments is one of the key means to prevent and control nosocomial infection and ensure the quality of medical care. It can be said that without excellent medical instrument disinfection and sterilization technology, there will be no development of modern surgical technology. There is no guarantee that various invasive diagnostic and therapeutic techniques can be implemented

Method used

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  • A kind of indole drug molecule for medical care, sterilization and disinfection, its preparation method and application
  • A kind of indole drug molecule for medical care, sterilization and disinfection, its preparation method and application
  • A kind of indole drug molecule for medical care, sterilization and disinfection, its preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029]

[0030] In a reaction flask with argon protection, add 1.1g of 3-aminopropyne and 1.5g of isatin into 50mL of N,N-dimethylformamide, stir to dissolve completely, and then add cuprous bromide 0.15g, cesium carbonate 3.2g and o-phenanthroline 0.36g, heated to 90°C under argon protection, reacted for 0.5h, poured into 100mL of water, extracted several times with 20mL of dichloromethane, combined the organic phases, concentrated After purification by column chromatography, 1.71 g of the alkynyl compound was obtained; LC-MS (ESI): m / z 185 [M+H] + ;Elemental analysis calculated value [C 11 h 8 N 2 O]: C, 71.73; H, 4.38; N, 15.21. Found: C, 71.68; H, 4.36; N, 15.25.

Embodiment 2

[0032]

[0033] Add 18.5g of alkynyl compound and 15.5g of phosphorus oxychloride to 400mL of chloroform in a reaction bottle with argon protection, heat to reflux for 2h, then wash the reaction liquid with water, separate the organic phase, concentrate and add 50mL of phenol and xylene 450mL, stir and dissolve, add potassium hydroxide 11g, heat to reflux, remove the moisture in the reaction system through a water separator, then add ammonium acetate 15g, continue to heat to reflux, react for 3h, slowly drop to room temperature, and then Pour the reaction solution into 500mL of water, extract it several times with 200mL of ethyl acetate, combine the organic phases, adjust the pH of the organic phase to neutral with dilute hydrochloric acid, then adjust the pH to 8-9 with saturated potassium hydroxide solution, and divide again. The organic phase was taken out, concentrated and separated by silica gel column chromatography to obtain 9.3 g of amine compounds; LC-MS (ESI): m / z ...

Embodiment 3

[0035]

[0036] In a reaction flask with nitrogen protection, add 18.5g of alkynyl compound and 24g of phosphorus oxychloride to 600mL of chloroform, heat to reflux for 3h, then wash the reaction solution with water, separate the organic phase, add 50mL of phenol and In 500mL of xylene, stir and dissolve, add 16g of potassium hydroxide, heat to reflux, remove the moisture in the reaction system through a water separator, then add 15g of ammonium acetate, continue to heat to reflux, react for 4h, slowly drop to room temperature, and then Pour the reaction liquid into 500mL of water, extract it several times with 200mL of ethyl acetate, combine the organic phase, adjust the pH of the organic phase to neutral with dilute hydrochloric acid, then adjust the pH to 8-9 with saturated potassium hydroxide solution, and separate The organic phase was concentrated and separated by silica gel column chromatography to obtain 17.69 g of amine compounds; LC-MS (ESI): m / z 184 [M+H] + ; 1 ...

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Abstract

The invention discloses an indole drug molecule for medical care, sterilization and disinfection, a preparation method and application thereof, and belongs to the technical field of synthesis of antibacterial drugs. The key points of the technical scheme of the present invention are: the indole drug molecule has a structure wherein R is the active carbonyl of isatin and 3-aminopropyne condensation in the present invention, and then the amide carbonyl is aminated, and the polyphosphoric acid ring is used to A novel indole compound was synthesized, and then its phenyl group was modified to obtain triazole and azole compounds. It is found that the target compound has a certain inhibitory effect on Staphylococcus aureus, and has the potential as an antibacterial drug.

Description

technical field [0001] The invention belongs to the technical field of antibacterial drug synthesis, and in particular relates to an indole drug molecule for sterilization and disinfection for medical care and its preparation method and application. Background technique [0002] The number of heterocyclic compounds is particularly large, widely distributed in nature, and plays an important role in the development and growth of organisms. At the beginning of the nineteenth century, the acquisition of heterocyclic compounds was mostly the extraction of natural products, but the yield of the obtained compounds was very low, the purity was not high, and the price was expensive; with the development of organic synthesis technology, in order to make full use of heterocyclic compounds , chemists began to carry out large-scale artificial synthesis of heterocyclic compounds, which have been widely used, including biomedicine, energy storage materials, biomimetic materials, high-perfo...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D487/04A61P31/04A01N43/90A01P1/00
CPCC07D487/04A61P31/04A01N43/90
Inventor 武婕姚玉娇景东帅魏俊逸董萌萌樊梦
Owner THE FIRST AFFILIATED HOSPITAL OF HENAN UNIV OF SCI & TECH
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