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Anti-hepatitis B virus tertiary amine oxide and preparation method and uses for manufacturing drug

A tertiary amine oxide and anti-hepatitis B technology, which is applied in antiviral agents, drug combinations, medical preparations containing active ingredients, etc., can solve the problems of expensive drugs and achieve low preparation costs and simple synthetic routes

Inactive Publication Date: 2006-02-15
TIANJIN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] One of the disadvantages of the above antiviral drugs is the high cost of the drugs

Method used

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  • Anti-hepatitis B virus tertiary amine oxide and preparation method and uses for manufacturing drug
  • Anti-hepatitis B virus tertiary amine oxide and preparation method and uses for manufacturing drug
  • Anti-hepatitis B virus tertiary amine oxide and preparation method and uses for manufacturing drug

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0057] Embodiment 1: the synthesis of N-phenyl-N-(3-dimethylaminopropyl) acetamide

[0058] Take 15mL DMSO, weigh 0.500g acetanilide, add to a 50mL round bottom flask, add 0.279g70% sodium hydride in batches, stir at room temperature for 0.5 hours, then add 0.704g N,N-dimethylamino-3-chloropropane salt The acid salt was added to the above mixture under vigorous stirring. After stirring at room temperature for 1 hour, the reaction system was heated in an oil bath, and the temperature was slowly raised to 70 degrees. After 5 hours, it was cooled to room temperature, and 100 mL of water was added to the reaction system. Extract with methane, combine the organic layers, wash the organic layer several times with water, dry the organic layer with anhydrous sodium sulfate sufficiently, remove the solvent under reduced pressure to obtain a crude product, dissolve the crude product in 10% dilute hydrochloric acid, wash with ethyl acetate, discard The ethyl acetate layer and the aqueous...

Embodiment 2

[0059] Embodiment 2: the synthesis of N-(3-dimethylaminopropyl) cyclocaprolactam

[0060] Take 15mL DMSO, weigh 2.000g cyclocaprolactam, add it to a 50mL round bottom flask, add 0.934g70% sodium hydride in batches, stir at room temperature for 0.5 hours, then add 3.356g N,N-dimethylamino-3-chloropropane salt The acid salt was added to the above mixture under vigorous stirring. After stirring at room temperature for 1 hour, the reaction system was heated in an oil bath, and the temperature was slowly raised to 80 degrees. After 8 hours, it was cooled to room temperature, and 100 mL of water was added to the reaction system. Extract with methane, combine the organic layers, wash the organic layer several times with water, dry the organic layer with anhydrous sodium sulfate sufficiently, remove the solvent under reduced pressure to obtain a crude product, dissolve the crude product in 10% dilute hydrochloric acid, wash with ethyl acetate, discard The ethyl acetate layer and the a...

Embodiment 3

[0061] Embodiment 3: the synthesis of N-n-butyl-N-(3-dimethylaminopropyl) acetamide

[0062] Take 15mL DMSO, weigh 2.000g N-n-butylacetamide, add it to a 50mL round bottom flask, add 1.282g70% sodium hydride, stir at room temperature for 0.5 hours, then add 3.223g N, N-dimethylamino-3- Chloropropane hydrochloride was added to the above mixture under vigorous stirring. After stirring at room temperature for 1 hour, the reaction system was heated in an oil bath, and the temperature was slowly raised to 60 degrees. After 9 hours, it was cooled to room temperature, and 100 mL of water was added to the reaction system. Extract with dichloromethane, combine the organic layers, wash the organic layer with water for several times, and dry thoroughly with anhydrous sodium sulfate, remove the solvent under reduced pressure to obtain a crude product, dissolve the crude product in 10% dilute hydrochloric acid, and wash with ethyl acetate , discard the ethyl acetate layer, adjust the pH of...

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Abstract

The invention relates to an anti-hepatitis B virus tertiary amine oxide and preparation method and uses for manufacturing drugs, wherein the tertiary amine oxidate has a structure represented by general formula (I) and (II), its preparing process comprises the compound having general formula (I) is prepared through condensation of derivatives of amine with acidamide and further oxidation, the compound having general formula (II) is prepared through the condensation between mono-hydrocarbyl piperazidine with carboxylic acid or carboxylic acid derivatives, or through alkylation of piperazine amidos and further oxidization. The compound can be used for preparing medicament for preventing or treating hepatitis B virus related diseases.

Description

technical field [0001] The invention relates to an anti-hepatitis B virus tertiary amine oxide, a preparation method and an application for preparing medicines, belonging to anti-hepatitis B virus compounds and its synthesis method and application. Background technique [0002] Hepatitis B is a disease that seriously endangers human health. At present, there are 2 billion people in the world under the threat of hepatitis B virus, and the total number of chronic hepatitis B patients is nearly 400 million. In my country, hepatitis B is one of the infectious diseases with a high incidence rate. There are more than 1 chronic hepatitis B virus carriers in my country, more than 30 million chronic hepatitis B patients, and one million chronic hepatitis B patients in the United States. However, there has been no fundamental breakthrough in the control and treatment of hepatitis B for a long time. [0003] At present, the anti-chronic hepatitis B drugs recognized by domestic and fo...

Claims

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Application Information

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IPC IPC(8): C07C233/35C07D241/04C07D223/10A61K31/16A61K31/495A61P31/20A61P1/16
Inventor 李春葆宴季丹赵鹏英张武军黎杰李享李大昌
Owner TIANJIN UNIV
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