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Process for preparing cytisine from thermopsis lanceolata glasses and seeds

A technology for the preparation process of Magus bean grass, applied in the direction of organic chemistry, etc., can solve the problems of product purity and yield not meeting the requirements of the pharmaceutical industry, not having mass production practicability, and staying in the laboratory, etc., to achieve product purity. The effect of high, low cost and simple preparation process

Inactive Publication Date: 2014-06-18
NINGXIA BAUHINIA PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Cynicine has very high medicinal value, and its industrial preparation method is not much reported in the patent literature, and the specific operation can only stay in the laboratory, which does not have the practicability of mass production, and the product purity and yield have reached It does not meet the requirements of the pharmaceutical industry, so there is a lot of room for innovation in the research and process of cydidine

Method used

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  • Process for preparing cytisine from thermopsis lanceolata glasses and seeds

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] Grind the dried rambean grass into coarse powder or break rambean seeds, weigh 100kg of rambean grass powder or 100kg of broken rambean seeds, put it into an extraction container, and moisten it with 3% sodium hydroxide solution After 7 hours, add chloroform to reflux for extraction, combine the extracts, and concentrate under reduced pressure to recover chloroform, then add ethanol for dissolution, and the solution is decolorized by alumina (Al 2 o 3 ), filtered, recovered ethanol under reduced pressure, added acetone to crystallize to obtain 8.2 kg of crude cydidine, and then recrystallized with petroleum ether to obtain 6.6 kg of cydidine fine product, with a content of 98.5%.

Embodiment 2

[0025] Grind the dried herb bean grass into coarse powder or crush herb bean seeds, weigh 120kg of herb bean grass powder or 120kg of broken herb bean seeds, put them into an extraction container, moisten with 2% potassium hydroxide solution After wetting for 8 hours, add chloroform to reflux for extraction, combine the extracts, and concentrate under reduced pressure to recover chloroform; add ethanol to dissolve, and the solution is decolorized by alumina (Al 2 o 3 ), filtered, recovered ethanol under reduced pressure, added acetone to crystallize to obtain 9.8 kg of crude cydidine, and then recrystallized with petroleum ether to obtain 7.9 kg of cydidine fine product, with a content of 98.8%.

Embodiment 3

[0027] Grind the dried herb bean grass into coarse powder or crush herb bean seeds, weigh 100kg of herb bean grass powder or 100kg of broken herb bean seeds, put them into an extraction container, and moisten them with 3% sodium hydroxide solution After wetting for 6 hours, add chloroform to reflux for extraction, combine the extracts, and concentrate under reduced pressure to recover chloroform; add ethanol to dissolve, decolorize the solution through activated carbon, filter, recover ethanol under reduced pressure, add acetone to crystallize to obtain 8.0 kg of crude cylindine, Add diethyl ether and recrystallize to obtain 6.4kg of cydidine fine product, the content of which is 98.0%.

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Abstract

The present invention provides a process for preparing cytisine from thermopsis lanceolata glasses or seeds. The process comprises: crushing thermopsis lanceolata glasses into coarse powder (1-3 cm) or breaking thermopsis lanceolata seeds, weighing a certain amount of thermopsis lanceolata glass coarse powder or broken thermopsis lanceolata seeds, adding an alkaline solution to moisten for 6-8 h, adding chloroform to carry out reflux extraction, mixing the extraction solutions, carrying out reduced pressure concentration to recover the chloroform, adding ethanol to dissolve, adopting a decoloration agent to carry out decoloration, filtering, carrying out reduced pressure recovery of ethanol, adding acetone to carry out crystallization to obtain a cytisine crude product, and adding petroleum ether to carry out re-crystallization to obtain the cytisine fine product. The process method has characteristics of simpleness, practicality, low cost and high purity, and is suitable for industrial production.

Description

technical field [0001] The invention relates to a process for preparing cydidine from sage bean grass and seeds. Background technique [0002] Cytisine, also known as cytisine and alkaloid, is an alkaloid extracted and separated from the whole grass and seeds of the dicotyledonous plant lanceolus Huanghua, and is the main active ingredient of Chinese herbal medicine. . The molecular formula is: C 11 h 14 N 2 O, is rhombohedral prism yellow-white powder. Pharmacological action: 0.15% cydidine aqueous solution is used clinically for intramuscular or intravenous injection to rescue reflex apnea, shock and neonatal asphyxia caused by surgery and various traumas. Recent studies have shown that this type of alkaloid also has various pharmacological effects such as respiratory stimulation, pressurization of cerebral circulation, anti-arrhythmia, anti-microbial infection, anti-ulcer, and increase of white blood cells. Strong anticancer activity. [0003] Through pharmacol...

Claims

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Application Information

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IPC IPC(8): C07D471/18
CPCC07D471/18
Inventor 白锋云张勇汪晓东
Owner NINGXIA BAUHINIA PHARMA
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