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New artemisinin extraction process

A technology of artemisinin and Artemisia annua, applied in the direction of organic chemistry, can solve the problems of high cost, incapable production, and difficulty in ready-made industrial scale, and achieve high recovery rate and low energy consumption

Active Publication Date: 2013-11-27
HUNAN HEALTHWARE BIOTECH LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

First, Academician Zhou Weishan of the Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences was the first to complete the research on the total synthesis of artemisinin (Zhou Weishan, Huang Dazhong, etc., Acta Chemie Sinica, 1989 (47): 710-715), in 2003 J.S.Yadav et al. (J.S.Yadav, R.Satheesh Babu and G. Sabitha. Stereoselective total synthesis of(+)-artemisinin, Tetrahedron Letters, 2003(44): 387-389) also completed the total synthesis of artemisinin, but their steps were all over 7 steps, and the total output The rate is less than 10%, the process is complicated and has no industrial value
The second is the current research hotspot, artemisinin, an intermediate of artemisinin produced by fermentation, and then semi-synthesized to obtain artemisinin (Shalini Bharel, Anamika Gulat. Enzymatic Synthesis of Artemisinin from Natural and Synthetic Precursors. Nat. Prod. 1998, 61, 633-636; EP2289897Al Photochemical process for producing artemisinin; WO2013 / 030247Al Method and device for the synthesis of artemisinin), but the current cost of this route method is still too high, and industrial scale is also difficult to be ready-made
The disadvantage of this type of method is that the extraction recovery rate is generally not high, between 85-90%, the quality of artemisinin varies greatly, and a large amount of high-risk solvents and silica gel are used
Another type of extraction and separation method is supercritical CO 2 Method (Qian Guoping, Yang Yiwen. Supercritical CO 2 Research on extracting artemisinin from Artemisia annua, Progress in Chemical Industry, 2005, 24: 286-291; WO2009 / 040119A2Process for manufacturing artemisinin), the disadvantage of this method is that the scale of the equipment is small, the production cannot be increased, and the final cost is also high , not suitable for industrial production

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0014] Example 1 Extracting artemisinin from dried Artemisia annua leaves

[0015] In a 2000mL three-neck bottle, add 100g of dried Artemisia annua leaves, add saturated ethyl acetate: ethanol: water = 10:2:88 system 800mL, this system contains 1‰ of polyethylene glycol, soak for 2h, and then at room temperature , Ultrasonic extraction 3h, power 90W. Ultrasonic extraction is completed, and the extract is obtained by filtration and stored. Continue to repeat the extraction twice according to the above method, the second extraction is combined with the first extraction, and the third extraction is applied to the next new extraction. Take a small amount of grass dregs that have been extracted three times, and use 10 times the amount of methanol for ultrasonic extraction for 30 minutes, power 90W, high-performance liquid phase detection, and calculate the artemisinin content in the grass to be less than 0.1‰, which is considered to be completely extracted. The combined extracts ...

Embodiment 2

[0016] Example 2 Extracting artemisinin from dried Artemisia annua leaves

[0017] In a 2000mL three-necked bottle, add 100g of dried Artemisia annua leaves, add saturated ethyl acetate: dichloromethane: water = 7:5:88 system 900mL, this system contains 2‰ of polyethylene glycol, soak for 2h, and then At room temperature, ultrasonic extraction was performed for 4 hours with a power of 70W. Ultrasonic extraction is completed, and the extract is obtained by filtration and stored. Continue to repeat the extraction twice according to the above method, the second extraction is combined with the first extraction, and the third extraction is applied to the next new extraction. Take a small amount of grass dregs that have been extracted three times, and use 10 times the amount of methanol for ultrasonic extraction for 30 minutes, power 90W, high-performance liquid phase detection, and the calculated artemisinin content in the grass is less than 0.1‰, which is considered to be complet...

Embodiment 3

[0018] Example 3 Extracting artemisinin from dried Artemisia annua leaves

[0019] In a 2000mL three-necked bottle, add 100g of dried Artemisia annua leaves, add saturated ethyl acetate: acetone: water = 7:3:90 system 1000mL, this system contains 2‰ of polyethylene glycol, soak for 2h, and then at room temperature , Ultrasonic extraction 4h, power 90W. Ultrasonic extraction is completed, and the extract is obtained by filtration and stored. Continue to repeat the extraction twice according to the above method, the second extraction is combined with the first extraction, and the third extraction is applied to the next new extraction. Take a small amount of grass dregs that have been extracted three times, and use 10 times the amount of methanol for ultrasonic extraction for 30 minutes, power 90W, high-performance liquid phase detection, and the calculated artemisinin content in the grass is less than 0.1‰, which is considered to be completely extracted. The combined extracts ...

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PUM

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Abstract

The invention relates to a simple process for extracting artemisinin from artemisa apiacea. The process comprises: placing dried artemisa apiacea leaf in a 3-mouthed bottle as a raw material, adding a solvent / water mixing system, soaking for 1-2 h, carrying out ultrasonic assisted extraction for 2-4 h, and repeating the extraction two times, wherein the third extraction solution is mechanically applied, the mixed extraction solution is used for the next separation and purification processes, and high-performance liquid chromatography detection results show that an extraction recovery rate is more than 98%. The method has characteristics of simple process and simple operation.

Description

technical field [0001] The invention relates to a new extraction process of natural antimalarial medicine raw material artemisinin. Background technique [0002] Artemisinin is a new type of sesquiterpene compound with a peroxy ring and a lactone ring. This special peroxy structure makes artemisinin have a wide range of biological activities, and early discovery of anti-malarial activity, anti-parasitic Insect activity, antibacterial, antipyretic and other activities, recently American scientists found that it has good anticancer activity, especially for breast cancer and ovarian cancer. Artemisinin was first extracted and isolated by the research group of Professor Tu Youyou of the Chinese Academy of Military Medical Sciences, and was used in anti-malarial research. It was successfully developed in the 1980s and became a new drug with independent intellectual property rights in my country. Artemisinin and a series of more active artemisinin derivatives developed later, art...

Claims

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Application Information

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IPC IPC(8): C07D493/20
Inventor 彭学东张梅赵金召闫勇义
Owner HUNAN HEALTHWARE BIOTECH LTD
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