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Azepine brazilin compound and synthesis method thereof

A compound, hematoxylin technology, applied in the fields of organic chemistry, drug combination, pharmaceutical formulations, etc., can solve the problems of weak biological activity and lack of medicinal value.

Inactive Publication Date: 2010-08-11
YUNNAN UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, its biological activity is not strong enough to reach the medicinal value

Method used

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  • Azepine brazilin compound and synthesis method thereof
  • Azepine brazilin compound and synthesis method thereof
  • Azepine brazilin compound and synthesis method thereof

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Embodiment Construction

[0045] The typical compounds of the present invention are listed below in conjunction with the embodiments, but the present invention is not limited to these examples or limited by these examples and their typical compounds.

[0046]

[0047] The preparation process of compound 1 is as follows:

[0048]Dissolve 41.6g (0.20mol) of 3,4-dimethoxycinnamic acid in 200ml of ethyl acetate, add 250-500mg of Pd / C (10%), hydrogenate in a water bath at 45°C for 10 hours at normal pressure, filter, The solvent was removed under reduced pressure, and ethyl acetate was recrystallized to obtain white crystals with a melting point of 97-98°C and a total yield of 79-92%.

[0049] Elemental analysis (C 11 h 14 o 4 )

[0050] Calculated (%): C, 62.85; H, 6.71;

[0051] Found (%): C, 62.38; H, 6.43.

[0052] Compound 2

[0053] The preparation process of compound 2 is as follows:

[0054] 10.5 g (0.05 mol) of hydrogenated 3,4-dimethoxycinnamic acid was dissolved in 200 ml of anhydrou...

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Abstract

The invention relates to an azepine brazilin compound and a synthesis method thereof. By using the structure of a natural product brazilin as a simulation object, a series of brazilin structure compounds containing nitrogen atoms are designed; and substituted cinnamic acid is used as a raw material, and a series of azepine brazilin compounds is obtained through serial chemical conversion and synthesis. Partial azepine brazilin compounds have strong anti-cancer activity, partial compounds have anti-HIV (Human Immunodeficiency Virus) activity, and partial compounds have aldose reductase suppressive activity and obviously reduce the blood sugar level. Medical compositions prepared from the compounds and at least one pharmaceutically acceptable excipient or carrier can be used for treating cancer and resist virus infections.

Description

technical field [0001] The invention relates to medicinal compounds in the field of medicinal chemistry, in particular to an azahematoxylin compound and a preparation method thereof. Background technique [0002] Cancer, metabolic diseases, and viral infections are diseases that seriously threaten human health. About 2 to 2.3 million cancer patients are newly discovered in my country every year. The incidence and mortality of cancer continue to rise along with people's life expectancy. The AIDS epidemic in China is serious, and the number of HIV-infected people ranks second in Asia and 14th in the world. According to expert estimates, the number of HIV infections in my country is increasing at an annual rate of 30%, which has become one of the most serious social problems in our country. Chronic hepatitis B is a chronic infectious disease caused by hepatitis B virus HBV, and is one of the main infectious diseases threatening human health. Globally, 1 million people die fro...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D221/18C07D491/056A61K31/473A61K31/4741A61P35/00A61P31/12A61P31/18A61P3/10
Inventor 张洪彬潘成学曾祥慧羊晓东刘建平李良
Owner YUNNAN UNIV
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