Genistein-3'-sodium sulfonate, dimethylation daidzein-3'-sodium sulfonate, their preparing process and pharmaceutical use

A technology for bis-methylated daidzein and genistein, which is used in drug combinations, pharmaceutical formulations, medical preparations containing active ingredients, etc., can solve the problem of low water solubility and fat solubility, affecting drug availability and effective time , large dosage and other problems, to achieve the effect of low production cost, good anti-hypoxia effect and simple process

Inactive Publication Date: 2006-09-20
SHAANXI NORMAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Genistein and daidzein belong to isoflavone compounds with low water solubility and fat solubility. When used as medicine, they can only be made into oral preparations and cannot be made into injections. Because of their low water solubility, they will affect the quality of the medicine Utilization and effective time, in order to achieve the purpose of treatment, in clinical use, patients take a large amount, and the therapeutic effect can only be observed after taking the medicine for 1 to 2 weeks

Method used

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  • Genistein-3'-sodium sulfonate, dimethylation daidzein-3'-sodium sulfonate, their preparing process and pharmaceutical use
  • Genistein-3'-sodium sulfonate, dimethylation daidzein-3'-sodium sulfonate, their preparing process and pharmaceutical use
  • Genistein-3'-sodium sulfonate, dimethylation daidzein-3'-sodium sulfonate, their preparing process and pharmaceutical use

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0048] In this example, first add genistein to the reaction kettle, stir with a mixer and gradually add solvent 80% sulfuric acid until the genistein is fully dissolved, then add the sulfonating agent concentrated sulfuric acid, the mole of genistein and sulfonating agent The ratio is 1:5. After stirring with a mixer, use a temperature regulating device to make the temperature of the reaction solution 60°C, and react for 5 hours to obtain a mixture of genistein-3'-sulfonic acid and unreacted raw materials. Cool to room temperature, add 10% sodium chloride aqueous solution with 5 times the total volume of the reactant, fully stirred, left to stand to precipitate a white precipitate, and filtered to obtain the crude product of genistein-3'-sodium sulfonate; Add 5 times the amount of 10% sodium chloride aqueous solution to the crude sodium sulfonate for purification to obtain the fine product of genistein-3'-sodium sulfonate (yield 85%).

[0049] Adopt the genistein-3 '-sodium su...

Embodiment 2

[0056] In this example, first add genistein to the reaction kettle, stir with a mixer and gradually add solvent 70% sulfuric acid until the genistein is fully dissolved, then add the sulfonating agent concentrated sulfuric acid, the mixture of genistein and sulfonating agent The molar ratio is 1:8. After stirring with a stirrer, the temperature of the reaction solution is set to 100°C with a thermostat, and the reaction is carried out for 5 minutes to obtain a mixture of genistein-3'-sulfonic acid and unreacted substances, which is cooled to room temperature. Add 5 times the volume of 10% sodium chloride aqueous solution, place it, and obtain white genistein-3'-sodium sulfonate precipitate, then separate genistein-3'-sodium sulfonate, and make it purified, separate and purify the raw materials used Be the 20% aqueous sodium chloride solution of 1 times of reactant total volume, other technological processes are identical with embodiment 1.

Embodiment 3

[0058] In this example, first add genistein to the reaction kettle, stir with a mixer and gradually add solvent 85% sulfuric acid until the genistein is fully dissolved, then add the sulfonating agent concentrated sulfuric acid, the mole of genistein and concentrated sulfuric acid The ratio is 1:3. After stirring with a mixer, use a thermostat to make the temperature of the reaction solution 20°C, and react for 10 hours to obtain a mixture of genistein-3'-sulfonic acid and unreacted substances. Add 5 times the volume of 10 % sodium chloride aqueous solution, place it, and obtain white genistein-3'-sodium sulfonate precipitate, then separate genistein-3'-sodium sulfonate, and make it purified, the raw materials used for separation and purification and the proportioning and implementation Example 1 is the same.

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Abstract

The invention provides a genistein-3'-sodium sulfonate, dimethylation daidzein-3'-sodium sulfonate and their preparing process comprising the steps of, charging reactants genistein or dismethylation daidzein into the dissolvent, charging sulphonating agent, subjecting the reactant and sulphonating agent to chemical reaction, separating the mixture by means of the conventional methods and purifying. The invention also provides a medicament and composition for treating cardiovascular and cerebrovascular diseases.

Description

technical field [0001] The invention belongs to the technical field of heterocyclic compounds, and specifically relates to a heterocyclic compound containing a six-membered ring without hydrogenation, with an oxygen atom as the only ring heteroatom, and fused with other rings. Background technique [0002] Soy isoflavones are natural extracts of soybeans, which bind to estrogen receptors and induce a class of phytochemicals with weak estrogen-like effects, among which genistein and daidzein are the main physiological functions. Genistein has obvious effects of anti-tumor, lowering blood fat, anti-atherosclerosis and improving women's menopausal symptoms. In recent years, genistein is also a nutritional ingredient that has been extensively studied. It has the functions of preventing tumors, regulating menstruation and other health benefits in the human body. Epidemiological studies have shown that the incidence of breast cancer and prostate cancer in East Asia is much lower ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D311/36A61K31/352A61P9/10A61P3/06
Inventor 张尊听刘谦光郑建斌索志荣薛东李发荣
Owner SHAANXI NORMAL UNIV
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