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A kind of compound and preparation method thereof

A technology of compounds and base catalysts, applied in the field of active compounds and their preparation, can solve problems such as reducing the toxicity of berberine, and achieve the effects of reducing toxicity and simple operation

Active Publication Date: 2018-01-09
BEIJING YISHENGTANG MEDICAL TECH RES CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] In addition, a large number of studies have shown that berberine is more toxic, but curcumin is basically non-toxic. Can the molecular nucleus of the two be spliced ​​together to reduce the toxicity of berberine?

Method used

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  • A kind of compound and preparation method thereof
  • A kind of compound and preparation method thereof
  • A kind of compound and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0062] An embodiment of the compound of the present invention, the chemical structural formula of the compound described in this embodiment is as attached figure 1 As shown, the compound described in this example is prepared by the following preparation method:

[0063] (1) Place the compound of formula (5) in a dry and clean three-necked flask, add DMAC to the three-necked flask, the molar ratio of DMAC to the compound of formula (5) is 5:1, and then heat and reflux in the electric jacket , the reaction temperature is 50-400°C, and the reaction is monitored by HPLC. When the basic reaction of the raw materials is complete or the product no longer increases, stop the reaction; when the temperature drops below 120°C, add pure ice water while stirring, and place it in the refrigerator Static crystallization, the temperature is about zero, then suction filtration, washing, and drying to obtain the compound of formula (1); in this step, the yield of the compound of formula (1) obt...

Embodiment 2

[0067] An embodiment of the compound of the present invention, the chemical structural formula of the compound described in this embodiment is as attached figure 1 As shown, the compound described in this example is prepared by the following preparation method:

[0068] (1) Place the compound of formula (5) in a dry and clean three-necked flask, add DMSO to the three-necked flask, the molar ratio of DMSO to the compound of formula (5) is 10:1, and then heat and reflux in the electric jacket , the reaction temperature is 50-400°C, and the reaction is monitored by HPLC. When the basic reaction of the raw materials is complete or the product no longer increases, stop the reaction; when the temperature drops below 120°C, add pure ice water while stirring, and place it in the refrigerator Static crystallization, the temperature is about zero, then suction filtration, washing, and drying to obtain the compound of formula (1); in this step, the yield of the compound of formula (1) ob...

Embodiment 3

[0072] An embodiment of the compound of the present invention, the chemical structural formula of the compound described in this embodiment is as attached figure 1 As shown, the compound described in this example is prepared by the following preparation method:

[0073] (1) Place the compound of formula (5) in a dry and clean three-necked flask, add DMF to the three-necked flask, the molar ratio of DMF to the compound of formula (5) is 15:1, and then heat and reflux in the electric jacket , the reaction temperature is 50-400°C, and the reaction is monitored by HPLC. When the basic reaction of the raw materials is complete or the product no longer increases, stop the reaction; when the temperature drops below 120°C, add pure ice water while stirring, and place it in the refrigerator Static crystallization, the temperature is about zero, then suction filtration, washing, and drying to obtain the compound of formula (1); in this step, the yield of the compound of formula (1) obta...

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Abstract

The invention discloses a compound. The compound is prepared from berberrubine and curcumin through a nucleophilic substitution reaction under certain conditions. According to the compound, the inventor is guided by the traditional Chinese medicine pair theory and the traditional Chinese medicine clinical medication experience, berberrubine and curcumin are purposefully and selectively combined through a specific synthetic method, and the obtained compound has the effects of increasing the effect and reducing toxins, and has better effects on the aspects of inflammatory resisting, tumor resisting, cancer resisting, hyperglycemia and hyperlipidemia reducing, bacterium resisting, cardiovascular and cerebrovascular disease resisting and the like. Meanwhile, the invention discloses a preparation method of the compound and application of the compound in preparing medicine for treating tumors, cancer, hyperglycemia, hyperlipidemia and the cardiovascular and cerebrovascular diseases.

Description

technical field [0001] The invention relates to a compound and a preparation method thereof, in particular to a compound with anti-inflammatory, anti-tumor, hypoglycemic and lipid-lowering, antibacterial and other effects and a preparation method thereof. Background technique [0002] Today, with the development of modern pharmacology, molecular biology and other theories and related science and technology, the ways and means of natural medicine development are constantly innovating. At present, there are roughly three ways to develop new drugs, namely the folk medicine way, the experience medicine way and the molecular way. Among them, with the development of molecular biology, genetics and information processing technology, molecular pathway has gradually become the main way to develop new drugs. However, based on the current national conditions of our country, and due to the limitations of technical equipment, at present, folk medicine and empirical medicine are the main...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D455/03A61P35/00A61P35/02A61P3/10A61P3/06A61P9/00A61P31/04A61P31/10
CPCC07D455/03
Inventor 李卫民冯毅凡朱贺年李铀张志朋
Owner BEIJING YISHENGTANG MEDICAL TECH RES CO LTD