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Method for synthesizing hypericin

A technology of hypericin and a synthesis method, which is applied in chemical instruments and methods, preparation of organic compounds, preparation of quinones, etc., can solve the problems of long reaction time, large environmental pollution, difficult purification of products, etc., and achieves relative yield and The effect of high purity, less environmental pollution and low preparation cost

Inactive Publication Date: 2011-07-20
WUHAN MAIDESEN MEDICAL TECH
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

The synthetic route disclosed in this document belongs to the traditional synthetic reaction process, which has the disadvantages of long reaction time, complex reaction components, large environmental pollution, troublesome operation and difficult purification of products.

Method used

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  • Method for synthesizing hypericin
  • Method for synthesizing hypericin
  • Method for synthesizing hypericin

Examples

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Embodiment Construction

[0019] The following are specific examples of the present invention, and further describe the technical solution of the present invention, but the protection scope of the present invention is not limited to these examples. All changes or equivalent substitutions that do not depart from the concept of the present invention are included in the protection scope of the present invention.

[0020] The methods used in the following examples are conventional methods unless otherwise specified.

[0021] Now use the method artificial synthesis hypericin of the present invention, concrete example comprises the following steps:

[0022] (1) Convert emodin into emodin anthrone

[0023] Get emodin 2g (7.4mmol), add in glacial acetic acid 120mL, Ar 2 protection, add SnCl under stirring 2 2H 2 O2.8g (12.4mmol), the mixture began to be heated, the reaction temperature reached 115°C, and reflux began to occur. At about 110°C, 48 mL of concentrated hydrochloric acid was added dropwise, and...

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Abstract

The invention relates to a method for synthesizing hypericin. The method comprises the following steps of: (1) dissolving emodin and SnCl2.2H2O in glacial acetic acid, raising the temperature to 100-125 DEG C, adding concentrated hydrochloric acid with the concentration of between 36 percent and 40 percent for reaction of 1-3 hours and cooling to obtain emodin anthrone; (2) dissolving emodin anthrone and potassium tert-butoxide in DMF (Dimethyl Formamide), carrying out reaction in a microwave solid-liquid phase synthesis / extraction instrument for 30-90 minutes and cooling to obtain protohypericin; and (3) dissolving the protohypericin in acetone, irradiating with a halogen lamp for 15-24 hours, concentrating and precipitating to obtain the hypericin. The method has the advantages of easiness in operating, low cost, little pollution, high yield, high purity and the like.

Description

technical field [0001] The invention belongs to the field of medicine synthesis and relates to a synthesis method of hypericin. Background technique [0002] Hypericin, that is, 4,4,5,5,7,7-hexahydroxy-2,2-dimethyl-middle-naphthodianthrone, is the belt of Hypericum perforatum of Garciniaceae The whole flower is processed and extracted, and it has a highly targeted and effective effect on viruses such as influenza. Hypericin has various pharmacological effects such as antiviral, antidepressant, sedative, antibacterial and anti-inflammatory, and wound astringent. It can inhibit DNA and RNA viruses, and also has a certain inhibitory effect on tumor cells. The multiple pharmacological effects of hypericin make its market demand increasing day by day. Since the content of hypericin in the whole plant of Hypericum perforatum is only about 4 / 10,000, at present, the content of hypericin extracted from Hypericum perforatum in its extracts at home and abroad does not exceed 1%. Ext...

Claims

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Application Information

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IPC IPC(8): C07C50/36C07C46/00
Inventor 刘明星王小利
Owner WUHAN MAIDESEN MEDICAL TECH
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