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9-(2-fatty ester ethoxy methyl) guanine, liposome, and preparation emthod

A technology of ethoxymethyl and fatty acid ester, which is applied in the field of pharmacy, can solve the problems of limited application and bioavailability of only 15%, and achieve the effect of economical purification method and simple synthesis method

Inactive Publication Date: 2005-01-12
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Clinically, it is mainly used to treat type 1 and type 2 herpes viruses, etc., and its bioavailability in the body is only 15%, which greatly limits its application

Method used

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  • 9-(2-fatty ester ethoxy methyl) guanine, liposome, and preparation emthod
  • 9-(2-fatty ester ethoxy methyl) guanine, liposome, and preparation emthod
  • 9-(2-fatty ester ethoxy methyl) guanine, liposome, and preparation emthod

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Example 1 Preparation of 9-(2-palmitate ethoxymethyl)guanine

[0032] (1) Synthesis of 9-(2-palmitate ethoxymethyl)guanine

[0033] Dissolve 2.252 g (10 mmol) of acyclovir in 80 ml of KOH-dried pyridine, stir and add 2.749 g of palmitoyl chloride (10 mmol), seal the above reaction solution in a water bath at 60° C. and stir for continuous reaction for 24 h. After the reaction was completed, 5 times the volume of deionized water was added, and the product was collected by filtration after cooling to room temperature.

[0034] (2) Purification of 9-(2-palmitate ethoxymethyl)guanine

[0035] Suspend the reaction product in 100ml of 0.01M HCl, stir for 30 minutes and then filter, suspend the filtered precipitate in 0.01M NaOH, stir for 10 minutes and then filter, wash the filtrate with 4°C deionized water, dissolve the filtrate with methanol at 60°C to saturation , and then cooled to 4°C to collect; repeat the above operation 5 times and then dry the precipitate to obtain...

Embodiment 2

[0040] Example 2 Preparation of 9-(2-myristate ethoxymethyl)guanine

[0041] (1) Synthesis of 9-(2-myristate ethoxymethyl)guanine

[0042] Dissolve 2.252 grams of acyclovir (10 mmol) in 80 ml of KOH-dried pyridine, add 2.749 grams of myristoyl chloride (10 mmol) to the above solution while stirring, and seal the above reaction solution in a water bath at 60°C and stir continuously. Reaction 24h. After the reaction was completed, 5 times the volume of deionized water was added, and the product was collected by filtration after cooling to room temperature.

[0043] (2) Purification of 9-(2-myristate ethoxymethyl)guanine

[0044] Suspend the reaction product in 100ml of 0.01M HCl, stir for 30 minutes and then filter, suspend the filtered precipitate in 0.01M NaOH, stir for 10 minutes and then filter, wash the filtrate with 4°C deionized water, dissolve the filtrate with methanol at 60°C to saturation , and then cooled to 4°C to collect; after repeating the above operation 5 time...

Embodiment 3

[0045] Example 3 Preparation of 9-(2-laurate ethoxymethyl)guanine

[0046] (1) Synthesis of 9-(2-laurate ethoxymethyl)guanine

[0047] Dissolve 2.252 g of acyclovir (10 mmol) in 80 ml of KOH-dried pyridine, stir and add 2.749 g of lauroyl chloride (10 mmol), seal the above reaction solution in a water bath at 60° C. and stir for continuous reaction for 24 h. After the reaction was completed, 5 times the volume of deionized water was added, and the product was collected by filtration after cooling to room temperature.

[0048] (2) Purification of 9-(2-laurate ethoxymethyl)guanine

[0049] Suspend the reaction product in 100ml of 0.01M HCl, stir for 30 minutes and then filter, suspend the filtered precipitate in 0.01M NaOH, stir for 10 minutes and then filter, wash the filtrate with 4°C deionized water, dissolve the filtrate with methanol at 60°C to saturation , then cooled to 4°C and collected; after repeating the above operation 5 times, the precipitate was dried to obtain 9...

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Abstract

This invention relates the prosome of Axilowei-9-(2-fatty acid ester ethoxy methyl) quanine and its liposome. In said invented product prodn. sodium deoxycholate method is used, with advantages of: simple synthesis method, economic and easy purification, high yield >70%, high pureness >99%, commercialization prodn. And experimental result shows that: said products have strong effect of anti-hepatitis B virus and anti-herpesvirus, better than their mother medicine-Axilowei.

Description

technical field [0001] The invention belongs to the field of pharmacy, and in particular relates to a class of prodrug 9-(2-fatty acid ester ethoxymethyl)guanine and liposome of acyclovir, and a preparation method thereof. Background technique [0002] Since Beijerinck first proposed the concept of viruses in 1898, the types of viruses have grown from dozens to more than 4,000 today. Especially in recent years, HIV virus, hepatitis B virus, SARS virus and avian influenza virus have caused extremely serious harm to public health all over the world, and have once again aroused the general attention of global antiviral drug research. However, the progress of antiviral drug research is relatively slow. According to reports, more than 30 kinds of drugs have been developed so far, and there are no real specific drugs for HIV virus, hepatitis B virus, SARS virus and avian influenza virus. The situation is extremely grim. [0003] Acyclovir (also known as acyclovir, chemical name: ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/522A61P31/22C07D473/18
Inventor 周珮蔡钦生黄海李继扬周伟
Owner FUDAN UNIV
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