Preparation method and applications of lamivudine twin drug

A technology of lamivudine and twin drugs, applied in the application of hepatitis therapeutic drugs, the field of preparation of lamivudine twin drugs, can solve problems such as inability to effectively alleviate liver fibrosis in patients, achieve easy preparation and quality control, Effects that are less complex and easy to apply

Inactive Publication Date: 2010-07-07
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Lamivudine cannot dissolve the fibroblasts in the liver interstitium, and can only indirectly delay the process of liver fibrosis. Therefore, it cannot effectively alleviate the liver fibrosis of patients. When lamivudine treats chronic hepatitis B, it is necessary to strengthen the anti-inflammatory effect. fibrosis treatment

Method used

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  • Preparation method and applications of lamivudine twin drug
  • Preparation method and applications of lamivudine twin drug
  • Preparation method and applications of lamivudine twin drug

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] Dissolve 5 g of ursolic acid in 125 ml of DMF, add 1.17 ml of ethyl chloroacetate (or equal mol of ethyl bromoacetate), K 2 CO 3 4.5 g, stirred at room temperature for 5 hours. The insoluble solid was removed by filtration, the filtrate was concentrated under reduced pressure, and 30ml×3 toluene was used to carry out DMF to obtain a pale yellow clear oily liquid, which was the esterification product, which was directly used in the next reaction without purification.

[0024] Add 30ml of 4NNaOHaq, 50ml of methanol, and 75ml of THF to the above oily liquid, stir to obtain a pale yellow clear liquid, and react with stirring at room temperature for 18 hours. Concentrate under reduced pressure to obtain a pale pink solid, add 90ml of water, adjust the pH to 3 with 4N NaOHaq, the solid turns white and thicker, add 75ml of chloroform, stir until the solid dissolves, separate the liquids, and extract the water with 70ml of chloroform Layers were combined and the chloroform la...

Embodiment 2

[0026] Add 3 g of the above-mentioned hydrolyzed product into 30 ml of DMF, stir to dissolve, control the external temperature at -15°C to -20°C, add 0.81 ml of triethylamine, slowly add 1.2 g of isobutyl chloroformate dropwise, after the addition is complete, keep stirring for 20 minutes. A white solid precipitated and was used in the next step without treatment.

[0027] A solution of 1.337 g of lamivudine and 1.2 ml of triethylamine in 15 ml of DMF was prepared, and slowly added dropwise to the above reaction solution at an external temperature of -15°C to -20°C. After the dropwise addition was completed, the mixture was incubated and stirred for 1 hour, then raised to room temperature, and stirred for 1 hour. The insoluble matter was filtered off, the filtrate was concentrated under reduced pressure, and 30ml×4 toluene was used to carry out DMF, and a white paste was obtained, which was the crude product. Add 75 ml of chloroform to the above crude product, shake in a wate...

Embodiment 3

[0029] Operation is with embodiment 1,2;

[0030] Embodiment 4 is the lamivudine-ursolic acid gemini drug (LMX-3) of linking group with 3-chloro (bromo) ethyl propionate

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Abstract

The invention provides a preparation method and applications of a lamivudine twin drug. Lamivudine, and ursolic acid or oleanolic acid are condensed into the lamivudine-ursolic acid or lamivudine-oleanolic acid twin drug at a low temperature by using ethyl chloroacetate (ethyl bromoacetate) or ethyl chloropropionate (ethyl bromopropionate) as the linking group. The twin drug possibly has a dual-action mechanism; and the twin drug has the action of antivirus, and also has the actions of resisting inflammations, protecting the liver cell membranes, improving the liver function and resisting fibrosis. Thus, the invention organically combines the antivirus therapy and the liver protection treatment and provides a new concept for the research and development of drugs for treating hepatitis.

Description

technical field [0001] The invention belongs to the field of pharmacy, and relates to a preparation method of a lamivudine gemini and the application of the gemini as a medicine for treating hepatitis. Background technique [0002] Nearly 2 billion people are infected by hepatitis B virus (HBV) in the world, and about 350 million of them are chronically infected with HBV. There may be more than 120 million chronic asymptomatic HBV carriers in my country. Because hepatitis B is extremely harmful to humans, about 1.2 million HBV-infected patients die of HBV-related diseases every year. The annual direct medical expenses for viral hepatitis in my country are as high as 30-50 billion yuan. Therefore, it is extremely urgent to develop safe and effective therapeutic drugs for HBV-infected patients all over the world, especially in my country. [0003] Drug therapy and gene therapy are mainly used in clinical anti-HBV. Drug therapy is the focus of clinical application, which is ma...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/56A61P1/16A61P31/20A61K31/513
Inventor 仲琰周建平霍美蓉
Owner CHINA PHARM UNIV
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