7-substitution-1-hero hydrogenated-2-ketone and ramification as well as its synthesizing method and usage

A technology of a heterohydronaphthalene and a synthesis method, which is applied in the field of synthesis of the compound 7-substituted-1-heterohydronaphthalene-2-one and its derivatives with anti-hepatitis B virus activity, can solve problems such as dissatisfaction, and achieves the Scientifically significant effect

Inactive Publication Date: 2003-07-23
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although the combination of drugs to regulate the host immune system and antiviral drugs can achieve better results, the treatment of hepatitis B is still not satisfactory

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Using 7-hydroxy-4-methyl-chromen-2-one as the starting material to react with N,N-dimethylthioformyl chloride, heat conversion reaction, and then hydrolyze with sodium methoxide to obtain 7-mercapto-4 -methyl-chromen-2-one, and finally alkylated with bromoethane to obtain the target compound 7-ethylthio-4-methyl-chromen-2-one.

Embodiment 2

[0024] Use 7-hydroxy-4-methyl-chromen-2-one as the starting material to react with tert-butanol, introduce tert-butyl and react with N,N-dimethylthioformyl chloride, then heat conversion reaction, Then hydrolyzed with sodium methoxide to obtain 7-mercapto-4-methyl-6-tert-butyl-chromen-2-one, and finally alkylated with dichloromethane to obtain a target compound 7-chloromethylsulfanyl-4- Methyl-6-tert-butyl-chromen-2-one.

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PUM

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Abstract

A compound 7-substitutent-1-naphthalene heterohydride-2-one and its derivatives, which has high activity to resist HBV, its preparing process, and its application in preparing medicine to treat hepatitis B are disclosed. Its advantage is higher suppression rate of HBsAg.

Description

technical field [0001] The invention belongs to the field of chemical pharmacy, and specifically relates to the synthesis method and anti-hepatitis B virus (HBV) activity of compound 7-substituted-1-heterohydronaphthalene-2-one and derivatives thereof. Background technique [0002] Hepatitis B virus (HBV, hepatitis B virus) is a 42nm relatively unique double-stranded DNA virus composed of an outer shell (HBsAg) and a core (HBcAg). HBV can be infected through blood transfusion, plasma, blood products or the use of virus-contaminated syringe needles, acupuncture needles, and blood collection equipment. Hemodialysis also has the risk of HBV infection. According to the detection results of hepatitis B in the population of various countries, it is estimated that there are about 350 million hepatitis B virus carriers in the world, which constitute an important source of infection and seriously threaten human health and life. Due to the particularity of the virus, the complexity o...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/366A61P1/16A61P31/12C07D215/22C07D311/06C07D335/06
Inventor 夏鹏陈瑛张倩张蓓娜郑筠青
Owner FUDAN UNIV
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