Preparation of matrine oxide

A technology for oxymatrine and preparation process, applied in the direction of organic chemistry and the like, can solve the problems of low yield, difficulty in large-scale industrial production, and high cost, and achieve the effects of simple preparation process, high product purity, and easy realization.

Inactive Publication Date: 2003-06-18
宁夏药物研究所(有限公司)
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

The traditional preparation process is to extract and separate oxymatrine from Sophora sophora, but its yield is very low, only 0.006%, and the extraction process is complicated, the cost is high, and it is difficult to realize large-scale industrial production. Moreover, at present, there is no one The preparation process can produce oxymatrine crystals with a purity of more than 99.9%
Therefore, the simple preparation of oxymatrine, and then the preparation of matrine injection, cannot be realized in technology, and it is not practical

Method used

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  • Preparation of matrine oxide

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Experimental program
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Effect test

Embodiment 1

[0044] Add 20 g of matrine into 15 g of hydrogen peroxide, react at 70° C. for 14 hours, and extract unreacted matrine with ether until there is basically no matrine in the reaction solution. Concentrate the reaction solution under reduced pressure, extract the concentrated solution under reduced pressure with chloroform, concentrate the extract under reduced pressure to obtain extract, dissolve and filter with ethanol, concentrate the filtrate under reduced pressure, add acetone to the concentrated solution to reflux, cool, precipitate crystals, and filter with suction , 15.5 g of crystals were obtained, which was oxymatrine.

Embodiment 2

[0046] 20 g of matrine was added to 15 g of hydrogen peroxide, stirred and reacted at 60° C. for 14 hours, and unreacted matrine was extracted with cyclohexane until there was basically no matrine in the reaction solution. After the reaction solution was concentrated under reduced pressure, it was extracted with chloroform, anhydrous sodium sulfate was added to the extract and dried and filtered, anhydrous ether was added to the filtrate, and 13 g of crystals were precipitated, which was oxymatrine.

Embodiment 3

[0048] 100 g of matrine was added to 75 g of hydrogen peroxide, stirred and reacted at 40° C. for 18 hours, and unreacted matrine was extracted with benzene until there was basically no matrine in the reaction solution. The reaction solution was concentrated under reduced pressure, extracted with chloroform, anhydrous ether was gradually added to the chloroform solution, and 90 g of a white solid was precipitated, which was oxymatrine.

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Abstract

The preparation of matrine oxide includes the reaction of matrine and hydrogen peroxide at 25-90 deg.c, the extraction of reacted solution or reduced pressure concentration and the reflux. The technological process is simple, practical, high in yield and suitable for industrial production.

Description

technical field [0001] The invention relates to a preparation process of oxymatrine extracted from matrine. Background technique [0002] Oxymatrine is one of the main alkaloids in the leguminous plant Sophora sophora, which has high medicinal value. Chinese patent CN1157717A discloses "Application of Oxymatrine in the Preparation and Treatment of Hepatitis B", which points out in the patent application that oxymatrine can be dissolved in pure distilled water without pyrogen deionization and formulated into matrine injection. But at the same time, it is pointed out that oxymatrine is a white solid extracted from Sophora flavescens and Sophora flavescens, and its molecular formula is C 15 h 24 o 2 , the purity is above 99%, and the balance is water. In actual preparation, it is impossible to achieve such a high purity, so it is not practical. Similarly, matrine injection prepared from oxymatrine cannot contain only one kind of alkaloid, so in actual operation, it is impo...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D471/22
Inventor 王忠效高斌景雁江黄建军葛青张树森冷晓红
Owner 宁夏药物研究所(有限公司)
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