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Acetylsalicylic acid-ethambutol heterocomplex as well as preparation method and application thereof

A technology of acetylsalicylic acid and ethambutol, which is applied in the field of acetylsalicylic acid-ethambutol hybrid compound and its preparation, and achieves the effects of abundant raw material sources, few side effects, and simple preparation method

Inactive Publication Date: 2019-01-18
WUHAN INSTITUTE OF TECHNOLOGY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, there are no relevant reports on the simple and efficient synthesis of acetylsalicylic acid-ethambutol hybrid drugs

Method used

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  • Acetylsalicylic acid-ethambutol heterocomplex as well as preparation method and application thereof
  • Acetylsalicylic acid-ethambutol heterocomplex as well as preparation method and application thereof
  • Acetylsalicylic acid-ethambutol heterocomplex as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Add 0.44g acetylsalicylic acid and 0.5g ethambutol to a 50mL single-necked flask, then add 15mL DMSO to dissolve completely, then add 0.5g DCC and 0.3g DMAP to the single-necked flask and stir evenly. The one-necked flask was placed on a collector-type constant-temperature heating magnetic stirrer, the temperature was raised to 30° C. and the reaction was stirred at a constant temperature, and the reaction was tracked with a thin-layer chromatography silica gel plate. After the reaction is finished, filter with a sand core funnel, slowly add the filtrate dropwise to 120 mL of water, and stir while adding. The obtained mixed solution was repeatedly extracted three times with dichloromethane, and the organic phase obtained by extraction was washed successively with water and saturated NaCl solution once respectively. Add anhydrous sodium sulfate to the washed organic phase for drying, and after standing for 0.5h, use a rotary evaporator (model RE-52C) to spin dry the orga...

Embodiment 2

[0027] Add 0.44g acetylsalicylic acid and 0.5g ethambutol to a 50mL single-necked flask, then add 15mL DMSO to dissolve completely, then add 0.5g DCC and 0.3g DMAP to the single-necked flask and stir evenly. The one-necked flask was placed on a collector-type constant temperature heating magnetic stirrer, the temperature was raised to 27° C. and the reaction was stirred at a constant temperature, and the reaction was tracked with a thin-layer chromatography silica gel plate. After the reaction is finished, filter with a sand core funnel, slowly add the filtrate dropwise to 135mL of water, and stir while adding. The obtained mixed solution was repeatedly extracted three times with dichloromethane, and the organic phase obtained by extraction was washed successively with water and saturated NaCl solution once respectively. Anhydrous sodium sulfate was added to the washed organic phase for drying, and after standing for 0.5 h, it was spin-dried with a rotary evaporator to obtain ...

Embodiment 3

[0029] Add 0.44g acetylsalicylic acid and 0.5g ethambutol to a 50mL single-necked flask, then add 15mL DMSO to dissolve completely, then add 0.5g DCC and 0.3g DMAP to the single-necked flask and stir evenly. The one-necked flask was placed on a collector-type constant-temperature heating magnetic stirrer, the temperature was raised to 33° C. and the reaction was stirred at a constant temperature, and the reaction was tracked with a thin-layer chromatography silica gel plate. After the reaction is finished, filter with a sand core funnel, slowly add the filtrate dropwise to 100 mL of water, and stir while adding. The obtained mixed solution was repeatedly extracted three times with dichloromethane, and the organic phase obtained by extraction was washed successively with water and saturated NaCl solution once respectively. Anhydrous sodium sulfate was added to the washed organic phase for drying, and after standing for 0.5 h, it was spin-dried with a rotary evaporator to obtain...

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Abstract

The invention relates to an acetylsalicylic acid-ethambutol heterocomplex as well as a preparation method thereof and application thereof in anti-tuberculosis. The chemical formula of the hybrid medicine is C19H30N2O5, and the molecular structure of the hybrid medicine is described in the description; during synthesis, the heterocomplex is obtained by enabling acetylsalicylic acid and ethambutol to be subjected to a reaction under the combined action of a dehydration condensing agent DCC and a catalyst DMAP. Compared with the traditional anti-tuberculosis medicines, the heterocomplex can act on different receptors at the same time, and has the advantages of being strong in activity, multiple in action sites, good in specificity, few in side effects, less in resistance to drugs, and the like; the heterocomplex also can reduce the corresponding toxic and side effects of the two medicines while improving the curative effect and enhancing the pharmacological action.

Description

technical field [0001] The invention relates to the technical field of drug synthesis, in particular to an acetylsalicylic acid-ethambutol hybrid compound and a preparation method and application thereof. Background technique [0002] Acetylsalicylic acid is one of the earliest, most widely used and most common antipyretic, analgesic and antirheumatic drugs. The effect is rapid, the drug effect is certain, the overdose is easy to diagnose and deal with, and allergic reactions rarely occur. Acetylsalicylic acid is often used to treat colds, fever, headache, neuralgia, joint pain, muscle pain, rheumatic fever, acute endogenous arthritis, rheumatoid arthritis and toothache, etc. It also has antithrombotic properties in the body and can reduce Formation of obstructive thrombi in peripheral arteries. In addition, acetylsalicylic acid can also inhibit the release reaction of platelets and the release of endogenous ADP, 5-HT, etc., and inhibit the second phase aggregation of plat...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C219/14C07C213/06A61P31/06
CPCC07C219/14A61P31/06C07C213/06
Inventor 祝宏李丽李爽李雪潘晓涵陈家宝
Owner WUHAN INSTITUTE OF TECHNOLOGY
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