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Hydrochloric acid 2-(1-ethyl propyl) moroxydine, preparation method and application thereof

A technology of ethylpropyl and morpholine guanidine, which is applied in the field of medicine, can solve the problems of unfavorable clinical application and high toxicity of morpholine guanidine hydrochloride, and achieve the effects of simple preparation method, low price and easy availability of raw materials

Inactive Publication Date: 2010-05-12
上海双科医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] Though above-mentioned morpholine hydrochloride is broad-spectrum antiviral drug, because morpholine hydrochloride toxicity is bigger, be unfavorable for clinical application; Therefore, in order to reduce its toxicity, strengthen its antiviral activity, the present invention makes morpholine hydrochloride into a new 2-(1-ethylpropyl) morpholine guanidine hydrochloride to improve the efficacy of the drug

Method used

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  • Hydrochloric acid 2-(1-ethyl propyl) moroxydine, preparation method and application thereof
  • Hydrochloric acid 2-(1-ethyl propyl) moroxydine, preparation method and application thereof
  • Hydrochloric acid 2-(1-ethyl propyl) moroxydine, preparation method and application thereof

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Embodiment 1

[0041] Embodiment 1 Preparation of 2-(1-ethylpropyl) morpholine guanidine hydrochloride

[0042] 1. Preparation of 2-(1-ethylpropyl)morpholine

[0043] Add 1mol of 2-(1-ethylpropyl)oxirane and 1mol of 2-aminoethanol into the reaction kettle, the reaction temperature is 40°C, stir, and react for 1.5 hours. After the reaction, obtain 1-ethanolamino by vacuum distillation -2-Ethyl-2-butanol.

[0044] Then add 1 mol of concentrated phosphoric acid and 1 mol of 1-ethanolamino-2-ethyl-2-butanol to the reaction kettle in sequence, stir at 50°C until the sample is completely melted, then heat to 65°C, add 3g of solid heteropoly Acid catalyst, stirred and reacted for 2 hours, opened the dehydration device to fractionate the water generated by the reaction; after the reaction was completed, cooled to room temperature, filtered; the solid heteropolyacid catalyst was recycled, and the filtrate was added to the reactor, and then 1mol 1-ethanolamino- 2-Ethyl-2-butanol neutralizes phosphor...

Embodiment 2

[0053] Embodiment 2 Preparation of 2-(1-ethylpropyl) morpholine guanidine hydrochloride

[0054] 1. Preparation of 2-(1-ethylpropyl)morpholine

[0055] Add 1mol of 2-(1-ethylpropyl)oxirane and 3mol of 2-aminoethanol into the reaction kettle, the reaction temperature is 50°C, stir, and react for 2.5 hours. After the reaction, obtain 1-ethanolamino by vacuum distillation -2-Ethyl-2-butanol.

[0056] Add 0.5 mol of concentrated phosphoric acid and 1 mol of 1-ethanolamino-2-ethyl-2-butanol to the reaction kettle in sequence, stir at 50°C until the sample is completely melted, then heat to 75°C, add 5g of solid heteropoly Acid catalyst, stirred and reacted for 3 hours, opened the dehydration device to fractionate the water generated by the reaction; after the reaction was completed, cooled to room temperature, filtered; the solid heteropolyacid catalyst was recycled, and the filtrate was added to the reactor, and then 0.5mol 1-ethanolamino- 2-Ethyl-2-butanol neutralizes phosphori...

Embodiment 3

[0059] Embodiment 3 Preparation of 2-(1-ethylpropyl) morpholine guanidine hydrochloride

[0060] 1. Preparation of 2-(1-ethylpropyl)morpholine

[0061] 2mol 2-(1-ethylpropyl)oxirane and 10mol 2-aminoethanol were added to the reaction kettle, the reaction temperature was 70°C, stirred, and reacted for 3.5 hours. After the reaction, 1-ethanolamino was obtained by vacuum distillation -2-Ethyl-2-butanol.

[0062] Add 0.5 mol of concentrated phosphoric acid and 1.5 mol of 1-ethanolamino-2-ethyl-2-butanol to the reaction kettle in sequence, stir at 80°C until the sample is completely melted, then heat to 95°C, add 7g of solid heteropoly Acid catalyst, stirred and reacted for 5 hours, opened the dehydration device to fractionate the water generated by the reaction; after the reaction was completed, cooled to room temperature, filtered; the solid heteropolyacid catalyst was recycled, and the filtrate was added to the reactor, and then 1mol 1-ethanolamino- 2-Ethyl-2-butanol neutraliz...

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Abstract

The invention provides a new hydrochloric acid 2-(1-ethyl propyl) moroxydine which can be obtained by chemical synthesis and has the advantages of low price of needed raw materials, easily obtained raw materials, simple and convenient preparation method, higher yield and suitability for industrialized production. The pharmacological activity experiment proves that compared with hydrochloric acid moroxydine, the hydrochloric acid 2-(1-ethyl propyl) moroxydine has the remarkably enhanced activity of in vivo resisting hepatitis B virus, hepatitis C virus, influenza virus, pneumovirus and herpes simplex virus, and the toxicity is one time lower than that of the hydrochloric acid moroxydine. Therefore, the new hydrochloric acid 2-(1-ethyl propyl) moroxydine can be applied to prepare antiviral drugs, especially anti-flu drugs, hepatitis C resisting drugs, hepatitis B resisting drugs, pneumovirus resisting drugs and herpes simplex viral keratitis resisting drugs.

Description

technical field [0001] The present invention relates to the field of medical technology, in particular to a new morpholine hydrochloride derivative, i.e. 2-(1-ethylpropyl) morpholine hydrochloride and its preparation method and application in the preparation of antiviral drugs, Especially in the preparation of anti-influenza drugs, anti-hepatitis C drugs, anti-hepatitis B drugs, anti-viral pneumonia drugs and anti-herpes simplex virus keratitis drugs. Background technique [0002] Viruses are the smallest of pathogenic microorganisms. They reproduce in cells. Their core is ribonucleic acid (RNA) or deoxyribonucleic acid (DNA). The outer shell is protein and does not have a cellular structure. Viruses are parasitic in host cells and rely on the host cell metabolic system for proliferation and replication. Viral nucleic acid and protein are synthesized under the control of genetic information provided by viral genes, and then assembled into mature infectious virions in the cy...

Claims

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Application Information

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IPC IPC(8): C07D265/30A61K31/5377A61P31/12
Inventor 徐从立黄山
Owner 上海双科医药科技有限公司
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