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Process of preparing 10-deacetyl Bakatin III from taxad branch and leaf residue

A technology of acetyl bacca and yew leaves, applied in chemical recovery, organic chemistry, etc., can solve the problems of difficulty in improving the purity, low yield of crystallization method, waste of resources, etc., and achieve environmental protection, low cost, The effect of simple process

Inactive Publication Date: 2003-02-26
SHANGHAI WANGU BIOLOGICAL SCI & TECH DEV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, we have found that after the leaves have been processed through the above process, a portion of 10-deacetylbaccatin III remains in the leaves, the general residual amount is 10-25%, which greatly wastes resources. In addition, the yield of the crystallization method is too low at one time. , its purity is not easy to improve, for this reason the present invention has to provide a new method

Method used

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  • Process of preparing 10-deacetyl Bakatin III from taxad branch and leaf residue
  • Process of preparing 10-deacetyl Bakatin III from taxad branch and leaf residue
  • Process of preparing 10-deacetyl Bakatin III from taxad branch and leaf residue

Examples

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Embodiment 1

[0023] like figure 1 , a scheme for the preparation of 10-desacetylbaccatin III. Take 1kg of the residue after paclitaxel was extracted from the leaves and branches of the planted yew, put it in a drying oven, heat it to 70°C and dry it under vacuum for 24 hours to obtain 927g of dry solid, grind it into 100 mesh powder, put it into a 5 liter wide mouth bottle, add 4 liters of water, soak in a water bath at 50°C for 4 hours, extract multiple times, combine the extracts, filter and concentrate, and spray dry to obtain 236g of powder, such as figure 2The high-performance liquid chromatography of the material obtained after the yew branch and leaf residue is boiled shows that it is 0.22g crude extract of 10-deacetylbaccatin III crystal, which is dissolved in 300ml ethyl acetate, and the sample is loaded by dry method. : 1 ethyl acetate and hexanaphthene rinse 30L, collect eluate segmentally, obtain the 10-deacetylbaccatin III crystal 0.22g that purity is 99.5%, see image 3 , ...

Embodiment 2

[0025] Take 1 kg of the residue after paclitaxel was extracted from the leaves and branches of the planted yew, put it in a drying oven and heat it to 70 ° C for 36 hours in vacuum to dry to obtain 911 g of dry solid, grind it into 100 mesh powder, put it into a 5 liter wide mouth bottle, add 4 liters of water, soak in 80°C water bath for 2 hours, extract multiple times, combine the extracts, filter and concentrate, spray dry to obtain 213g powder, dissolve in 300ml ethyl acetate, dry load, use 1:1 ethyl acetate Esters and cyclohexane rinsed 30 L, and the eluent was collected in sections to obtain 0.25 g of 10-deacetylbaccatin III crystals with a purity of 99.6%.

Embodiment 3

[0027] Take the leaves and branches of the planted Taxus chinensis and extract 10kg of the residue after paclitaxel is extracted, put it in a drying oven and heat it to 70°C for 36 hours in vacuum to dry to obtain 9217g of dry solid, grind it into a 100-mesh powder, put it into the extraction tank, add 45 liters of water, soaked in a water bath at 80°C for 3 hours, extracted several times, combined the extracts, filtered and concentrated, spray-dried to obtain 3215g powder, dissolved in 3L ethyl acetate, and applied dry method several times, using 1:1 ethyl acetate Rinse with cyclohexane, collect the eluent in sections, and obtain 2.98 g of 10-deacetylbaccatin III crystals with a purity of 99.7%.

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Abstract

A preparation process of 10-deacetyl Bakatin III from taxad branch and leaf residues after extracting taxol includes drying at normal temperature to 70 deg.C to eliminate organic solvent; soaking in water in an extracting tank; filtering to eliminate dregs while the soaked lquid is still hot; concentrating the filtrate to obtain coarse 10-deacetyl Bakatin III extractive; spray-drying the coarse extract to obtain dry power; dissolving the powder in ethyl acetate; chromatographic separation; gradient leaching with ethyl acetate and cyclohexane to collect the leached liquid as the 10-deacetyl Bakatin III product of over 99.5% purity. The present invention makes it possible to use waste resource.

Description

technical field [0001] The invention relates to a method for preparing 10-deacetyl baccatin III from the residue after planting yew leaf branches. Background technique [0002] 10-Deacetylbaccatin III (10-DABIII) is a natural organic compound isolated from Taxus chinensis, which is used to synthesize the anticancer drug paclitaxel or paclitaxel. Its molecular structure is as follows: Paclitaxel is also a natural organic compound found in the yew tree species. It has a strong killing effect on breast cancer, ovarian cancer, lung cancer and leukemia cells. One of the most popular anticancer drugs, the demand is increasing rapidly. But, the source of natural paclitaxel is extremely limited, and the content in bark is generally between 0.01%-0.03%; The growth of yew tree species is very slow, and the old tree of a growth hundred years can generally only strip off 25kg bark; To extract 1kg of pure paclitaxel for use by 12,000 cancer patients requires the bark of 30,000 yew tre...

Claims

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Application Information

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IPC IPC(8): C07D305/14
CPCY02P20/582
Inventor 陈建民李明李华周海燕
Owner SHANGHAI WANGU BIOLOGICAL SCI & TECH DEV
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