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Benzene acrylamide compound as well as preparation method and application thereof

A technology of phenylacrylamide and acrylamide, which is applied in the field of preparation of phenylacrylamide compounds, can solve the problems that infectious diseases cannot be completely cured, affect the efficacy of antibacterial drugs, and irrational use of antibiotics, etc.

Pending Publication Date: 2022-07-29
ZUNYI MEDICAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002] The irrational use of antibiotics has affected the efficacy of antibacterial drugs, and the emergence of multi-drug resistance is a serious threat to human health, resulting in many clinical infectious diseases that cannot be completely cured

Method used

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  • Benzene acrylamide compound as well as preparation method and application thereof
  • Benzene acrylamide compound as well as preparation method and application thereof
  • Benzene acrylamide compound as well as preparation method and application thereof

Examples

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Effect test

preparation example Construction

[0020] Preparation of compound II of the present invention:

[0021]

[0022] Wherein, EDCI is 1-ethyl-(3-dimethylaminopropyl) carbodiimide hydrochloride, and HOBT is 1-hydroxybenzotriazole.

Embodiment 1

[0024] Preparation of compound II-1: Weigh 0.400g (1.64mmol) osthole and 0.531g (9.83mmol) sodium methoxide respectively and add them to a 100mL reaction tube, then add 30mL absolute ethanol, stir to dissolve, heat to reflux, TLC tracking, After 60 hours of reaction, the solvent was concentrated by rotary evaporation, 20 mL of distilled water was added to the concentrated solution, extracted with ethyl acetate, the aqueous layer was adjusted to pH=2-3 with 1.0 mol / L HCl, extracted with ethyl acetate, and dried over anhydrous magnesium sulfate. , filtered with suction, concentrated the solvent, separated and purified by silica gel column chromatography to obtain intermediate I.

[0025] Take 0.040g (0.15mmol) of Intermediate I, 0.046g (0.31mmol) of HOBT, 0.06mL (0.46mmol) of triethylamine and 10mL of anhydrous dichloromethane into a 50mL three-neck flask, under ice bath, dropwise add 5mL of EDCI 0.058 g (0.31 mmol) dissolved in anhydrous dichloromethane was stirred for reaction...

Embodiment 2

[0027] Preparation of compound II-2: Weigh 0.400g (1.64mmol) osthole and 0.531g (9.83mmol) sodium methoxide respectively and add them to a 100mL reaction tube, then add 30mL anhydrous ethanol, stir to dissolve, heat to reflux, TLC tracking, After 60 hours of reaction, the solvent was concentrated by rotary evaporation, 20 mL of distilled water was added to the concentrated solution, extracted with ethyl acetate, the aqueous layer was adjusted to pH=2-3 with 1.0 mol / L HCl, extracted with ethyl acetate, and dried over anhydrous magnesium sulfate. , filtered with suction, concentrated the solvent, separated and purified by silica gel column chromatography to obtain intermediate I.

[0028] Take 0.040g (0.15mmol) of intermediate I, 0.045g (0.30mmol) of HOBT, 0.06mL (0.46mmol) of triethylamine and 10mL of anhydrous dichloromethane into a 50mL three-neck flask, under ice bath, dropwise add 5mL of EDCI 0.057 g (0.301 mmol) dissolved in anhydrous dichloromethane was stirred and the re...

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PUM

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Abstract

The invention discloses a preparation method of a phenylacrylamide compound shown in a general formula II in the technical field of organic chemistry. A substituent R of the phenylacrylamide compound is defined in the specification. The invention also relates to application of the compound shown in the general formula II in medicines for treating and / or preventing bacterial infection.

Description

technical field [0001] The invention relates to the field of organic chemistry, in particular to the preparation and application of a phenylacrylamide compound. Background technique [0002] The irrational use of antibiotics has affected the efficacy of antibacterial drugs, and the emergence of multi-drug resistance is a serious threat to human health, resulting in many clinical infectious diseases that cannot be completely cured. Therefore, new antimicrobial drugs are urgently needed to overcome these concerns. SUMMARY OF THE INVENTION [0003] The present invention aims to provide a phenylacrylamide compound that can replace antibiotics in clinical medicine and a preparation method thereof in view of the deficiencies in the current use of antibiotics. [0004] A phenylacrylamide compound (hereinafter referred to as compound II) in this scheme, its chemical structure is shown in general formula II: [0005] [0006] Wherein, R is a hydrocarbon group of 1 to 6 carbon ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C235/34C07C231/02C07D307/52A61P31/04
CPCC07C235/34C07D307/52A61P31/04Y02P20/55
Inventor 杨家强王启益董向涛吴学姣周绪容
Owner ZUNYI MEDICAL UNIVERSITY
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