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Method for full chemical synthesis of fibrauretin anti-bacterial anti-inflammatory medicine

A technology of medicine patellogenin, antibacterial and anti-inflammatory, applied in the direction of organic chemistry, etc., can solve the problems of high equipment requirements, low yield, and complicated operation.

Inactive Publication Date: 2012-07-04
广西中医学院
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This method has 10 steps in total, the conditions are harsh, the equipment requirements are high, the operation is cumbersome, the yield is low, the total yield is about 20%, and it is not suitable for industrialized large-scale production

Method used

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  • Method for full chemical synthesis of fibrauretin anti-bacterial anti-inflammatory medicine
  • Method for full chemical synthesis of fibrauretin anti-bacterial anti-inflammatory medicine
  • Method for full chemical synthesis of fibrauretin anti-bacterial anti-inflammatory medicine

Examples

Experimental program
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Effect test

Embodiment 1

[0027] (1) Synthesis of N-(3,4-dimethoxyethylphenyl)-C-(2,3-dimethoxyphenyl)imine 3

[0028] Add 3,4-dimethoxyphenethylamine and 2,3-dimethoxybenzaldehyde to the reaction bottle, and raise the temperature to 120°C for 4 hours under stirring. The product is not purified, and 3.01g of viscous reddish brown is obtained. liquid (3).

[0029] (2) Synthesis of N-(2,3-dimethoxybenzyl)-(3,4-dimethoxy)phenethylamine 4

[0030] After 3 was cooled to room temperature, methanol was added to dissolve, and sodium borohydride was added in portions under stirring at room temperature, and reflux was continued for 2 hours after addition, methanol was recovered, the residue was dissolved in water, extracted with ethyl acetate, anhydrous Na 2 SO 4 After drying, the solvent was recovered after filtration to obtain 2.88 g of yellow viscous liquid 4, and the pH value of the obtained product was adjusted with concentrated hydrochloric acid for later use.

[0031] Synthesis of target product palmat...

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Abstract

The invention discloses a method for full chemical synthesis of a fibrauretin anti-bacterial anti-inflammatory medicine. The method adopts 3,4-dimethoxyphenylethylamine and 2,3-dimethoxybenzaldehyde as initial raw material, and prepares a target product by three-step chemical reaction including heat condensation, sodium borohydride reduction and cyclization reaction. The full chemical synthesis method of fibrauretin in the invention has the advantages of simple reaction steps, mild reaction conditions, low cost and high yield, and is suitable for industrial production.

Description

technical field [0001] The invention relates to a total chemical synthesis method of the antibacterial and anti-inflammatory drug palmatine. Background technique [0002] Lutein is a quaternary ammonium alkaloid isolated from the roots and stems of the plant Fibrurea recisa Pierre. Staphylococcus aureus, Bacillus subtilis, Candida albicans and its drug-resistant bacteria, Candida glabrata, Candida parapsilosis, Candida krusei, Cryptococcus neoformans and other pathogenic bacteria and drug-resistant bacteria have broad-spectrum antibacterial effect. At present, palmatine has been widely used clinically in various types of infections and gynecological diseases, etc., and has good curative effect. It has been made into various types of preparations and put on the market, and the market demand is relatively large. However, due to the narrow distribution area of ​​yellow vine natural forests, the resources are facing exhaustion, and the artificially cultivated forests have not b...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D455/03
Inventor 卢汝梅霍丽妮陆桂枝阎莉韦建华朱小勇
Owner 广西中医学院
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