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Synthetic method of Myrioneuron faberi Hemsl. alkaloids

A synthetic method and the technology of veined wood, applied in the direction of organic chemistry, can solve the problems that hinder research and application, increase the difficulty of research in physiological and pharmacological activities, and achieve the effects of low loss, short chemical process and convenient operation

Inactive Publication Date: 2016-04-13
LANZHOU UNIVERSITY
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

This increases the difficulty of research on its physiological and pharmacological activities and hinders further research and application of the substance

Method used

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  • Synthetic method of Myrioneuron faberi Hemsl. alkaloids
  • Synthetic method of Myrioneuron faberi Hemsl. alkaloids
  • Synthetic method of Myrioneuron faberi Hemsl. alkaloids

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Embodiment Construction

[0029] The present invention provides a new method for preparing venaline A and B. The method uses acrolein as a starting material, and finally prepares acrolein A and B through 5 steps of chemical reactions, specifically comprising the following steps:

[0030] (1) Synthesis of compound 3

[0031]

[0032] Dissolve 5.6g (100mmol) of acrolein in 250ml of acetonitrile, add 18g (120mmol) of sodium iodide, slowly drop into 15.3ml (120mmol) of chlorotrimethylsilane, and react for 20 minutes. Subsequently, 6.7 ml (120 mmol) of ethylene glycol was slowly added dropwise, and the reaction was continued for 20 minutes. After the reaction is complete, add 100ml of 5% sodium bicarbonate aqueous solution to quench the reaction, add 100ml of petroleum ether, the system is divided into three phases, wash once with saturated sodium thiosulfate solution, and then wash several times with saturated brine until the system is divided into two phases. The upper organic phase was separated, dri...

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Abstract

Myrioneuron faberi Hemsl. alkaloids A and B and parts of derivatives thereof have a substantial inhibition effect on hepatic c viruses, and have lower cytotoxicity than a present hepatic c treatment drug telaprevir. Only 30mg of the Myrioneuron faberi Hemsl. alkaloid A and 2mg of the Myrioneuron faberi Hemsl. alkaloid B are separated from 30kg of Myrioneuron faberi Hemsl. plants, so the research difficulty of the physiological and pharmacological activities of the alkaloids is increased, and further researches and application of the above substances are obstructed. The invention provides a synthetic method of the Myrioneuron faberi Hemsl. alkaloids A and B to solve the disadvantage of obstruction of the further researches and application of the substances due to small obtaining amount of the Myrioneuron faberi Hemsl. alkaloids A and B. The method starts from the cheap and easily available raw material, realizes artificial synthesis of the Myrioneuron faberi Hemsl. alkaloids A and B for the first time, allows the Myrioneuron faberi Hemsl. alkaloids A and B to be continuously and massively synthesized, and provides good technical support for subsequent realization of large-scale production and structure activity relation researching of natural products.

Description

technical field [0001] The invention belongs to the technical field of organic synthesis, and in particular relates to a preparation method of eucalyptus alkaloids. Background technique [0002] Hepatitis C is a worldwide disease. According to the statistics of the World Health Organization, 130 million to 150 million people worldwide suffer from chronic hepatitis C infection. A large number of chronically infected people will develop liver cirrhosis or liver cancer, of which about 500,000 people per year Died of hepatitis C-related liver disease. However, the price of antiviral drugs to treat hepatitis C is very high, and people have been developing new drugs to ensure that more hepatitis C patients around the world are treated. [0003] In recent years, a large number of natural products with novel structures and significant activities have been isolated from plants of the genus Dendrobium, many of which can be used as lead compounds for new drug research. Myrifabral A (...

Claims

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Application Information

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IPC IPC(8): C07D491/18
CPCC07D491/18
Inventor 厍学功宋登鹏谢新刚
Owner LANZHOU UNIVERSITY