Staurosporine extraction method

A staurosporine and extraction method technology, applied in the field of separation and purification of chemicals, can solve the problems of poor quality staurosporine, content of only 89%, high production cost, etc., achieve short production cycle, easy to scale up, and good quality Effect

Active Publication Date: 2020-01-03
HUBEI HONCH PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] Among the methods disclosed in the above-mentioned patents, the extraction methods of US4107297 and US4973552 all adopt silica gel column chromatography, so the product quality is better, and the purity reaches more than 99%, but the production cost is high...

Method used

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Examples

Experimental program
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Embodiment 1

[0036] (1) Add 3% perlite (according to the volume of the fermentation broth, Kg / L) to the staurosporine fermentation broth, stir for 30 ± 5min, plate and frame filter, the filtrate is discharged to the sewage treatment station, and the filter cake is blown with compressed air Dry for 2±0.5h, collect the fungus residue;

[0037] (2) extract bacterium residue with organic solvent 3 times, add the solvent of 4 times volume (L / Kg bacterium residue) each time, filter, merge filtrate;

[0038] (3) The filtrate is concentrated under reduced pressure at a certain temperature to 1 / 30 of the original volume, adding an equal volume of solvent, an equal volume of aqueous solution, and 1 / 3 volume of extraction aid, stirring for 30 ± 10 min, and standing for 60 ± 10 min. Separate the liquid, extract the aqueous phase with the original volume of solvent once more, combine the organic layers, add 5% (Kg / L) anhydrous sodium sulfate, stir and dry for 60±10min, and filter;

[0039] (4) Concent...

Embodiment 2

[0043] (1) Add 9Kg perlite to 300L fermented liquid containing staurosporine 451mg / L, stir for 30±5min, plate and frame filter, discharge the filtrate to the sewage treatment station, dry the filter cake with compressed air for 2±0.5h, Get 62Kg of fungus residue;

[0044] (2) Put the fungus residue into a 500L mixing tank, add 250L of absolute ethanol, stir for 5±1h, filter out the extract, keep the fungus residue in the tank, add absolute ethanol to extract twice, 250L each time, combine filtrate;

[0045] (3) Concentrate the filtrate under reduced pressure at 50±5°C to 25-30L, add 30L chloroform, 30L 2% ammonia water, 10L anhydrous methanol, stir for 30±10min, let stand for 60±10min, separate liquid, water phase Extract once more with 30L chloroform, combine the organic layers, add 3Kg anhydrous sodium sulfate, stir and dry for 60±10min, and filter;

[0046] (4) Concentrate the filtrate to 3L under reduced pressure at 35±5°C, add 6L of anhydrous methanol, stir at room temp...

Embodiment 3

[0050] (1) Add 9Kg perlite to 300L fermented liquid containing staurosporine 408mg / L, stir for 30±5min, plate and frame filter, discharge the filtrate to the sewage treatment station, dry the filter cake with compressed air for 2±0.5h, Get 65Kg of fungus residue;

[0051] (2) Put the fungus residue into a 500L stirring tank, add 250L of acetone, stir for 5±1h, filter out the extract, keep the fungus residue in the tank, add acetone to extract twice, each time 250L, and combine the filtrate;

[0052] (3) Concentrate the filtrate to 25-30L under reduced pressure at 50±5°C, add 30L dichloromethane, 30L 3% sodium carbonate, 10L anhydrous methanol, stir for 30±10min, let stand for 60±10min, separate liquid, water The phase was extracted once more with 30L dichloromethane, the organic layers were combined, 3Kg anhydrous sodium sulfate was added, stirred and dried for 60±10min, and filtered;

[0053] (4) Concentrate the filtrate to 3L under reduced pressure at 35±5°C, add 6L of acet...

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Abstract

The invention discloses a staurosporine extraction method which comprises the following steps: 1) plate-frame filtration; 2) acetone extraction; 3) extraction; and 4) crystallization and vacuum drying. The staurosporine extraction method disclosed by the invention has advantages of low production cost, short extraction period, simple operation, stable method, easy amplification, and extremely highpractical value in industrial production.

Description

technical field [0001] The invention belongs to the field of separation and purification of chemicals, and in particular relates to a staurosporine extraction method. Background technique [0002] Staurosporine (staurosporine, STA, the following structural formula (1)) is a natural product with good pharmaceutical and biological activities. The compound was first obtained by Omura in 1997 as an indolecarbazole alkaloid isolated from soil actinomycetes. X-ray single-crystal diffraction analysis shows that the center is an indolecarbazole ring, the N below the ring is connected with a small molecular sugar, and the upper part is connected with a lactam ring. STA is a strong PKC inhibitor (IC50=2.7nM), which mainly acts on various kinases, topoisomerases and cell cycle regulatory factors in cell signal transduction pathways. [0003] The structurally modified staurosporine derivative midostaurin (structural formula (2)) was approved in 2017 for the treatment of newly diagnose...

Claims

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Application Information

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IPC IPC(8): C07D498/22
CPCC07D498/22
Inventor 付光明戴绪霖霍育生张文凯
Owner HUBEI HONCH PHARMA
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