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Method for preparing high-purity taxone compounds

A technology for taxanes and compounds, which is applied in the directions of organic chemistry, drug combination, pharmaceutical formulation, etc., can solve the problems of increasing production cost, polluting the environment, complicated operation and the like, and achieves the effects of low cost, little environmental pollution and easy operation.

Inactive Publication Date: 2008-05-14
SHANGHAI TECHWELL BIOPHARMACEUTICALS CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0013] However, these methods still have the following disadvantages: 1) the purity of paclitaxel is not high, and can not reach more than 99.9%; 2) the operation is relatively complicated; 3) a large amount of organic solvents need to be used, which pollutes the environment and improves production cost

Method used

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  • Method for preparing high-purity taxone compounds
  • Method for preparing high-purity taxone compounds
  • Method for preparing high-purity taxone compounds

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0103] Embodiment 1: the purification of paclitaxel

[0104] HPLC conditions for sample detection

[0105] Chromatograph: Waters high performance liquid chromatography system;

[0106] Chromatographic column: Waters Spherisorb ODS (24.6mm×150mm, 3μm);

[0107] Mobile phase A: water: acetonitrile (3:2);

[0108] Mobile phase B: acetonitrile;

[0109] program:

[0110] time

(minute)

mobile phase A

(%)

mobile phase B

(%)

0-20

100

0

20-60

100→10

0→90

60-62

10→100

90→0

62-70

100

0

[0111] Injection volume: 15μl;

[0112] Column temperature: 35°C;

[0113] Detection wavelength: 227nm;

[0114] Flow rate: 1.2ml / min.

[0115] Raw material description

[0116] The raw material used in this embodiment is commercially available paclitaxel with a purity of about 99% (its HPLC profile is as follows: figure 1 Shown), rel...

Embodiment 2

[0130] Embodiment 2: the purification of docetaxel

[0131] HPLC conditions for sample detection

[0132] Chromatograph: Waters high performance liquid chromatography system;

[0133] Chromatographic column: Waters Spherisorb ODS2 (4.6mm×150mm, 3μm);

[0134] Mobile phase: 0.043mol / L ammonium acetate solution: acetonitrile=45:55;

[0135] Injection volume: 20μl;

[0136] Column temperature: 35°C;

[0137] Detection wavelength: 232nm;

[0138] Flow rate: 1.0ml / min.

[0139] Purification process

[0140] 100 liters of AMBERLITE XAD 1600 resin (purchased from Rohm and Haas, USA) was loaded into a stainless steel chromatography column with a diameter of 400 mm and a height of 1100 mm, and the resin was washed with 100 liters of purified water.

[0141] Weigh 1000 g of docetaxel (purity 99.40%), dissolve it in 180 liters of 15% N,N-dimethylformamide (DMF) aqueous solution, and then load a sample at a flow rate of 70 liters / hour. After the sample is loaded, it is washed ...

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Abstract

The invention discloses a method for preparing taxol, docetaxel and other taxanes. The taxanes synthesized or semi-synthesized or extracted from the plants are used as the raw materials, the waterborne solvent is used to dissolve the materials, and the macroporous absorption resins such as Diaion Hp resins, Amberlite XAD resins are used as the stationery phase, the organic solvents such as THF, N, N-DMF and other solvents are used as the eluent, the atmospheric pressure column chromatography is adopted, one step is enough to extract the taxanes with the purity above 99.90% with high yield above 99.0%. The invention has the advantages of simple method, convenient operation, favorableness to production expansion, small amount and recyclability of organic solvent and environmental friendliness.

Description

technical field [0001] The invention relates to a method for processing taxane compound raw materials. More specifically, the present invention relates to a method for preparing taxane compounds with high purity by using macroporous adsorption resin chromatography to treat raw materials of taxane compounds. Background technique [0002] Taxane compounds are a class of compounds extracted from the bark, roots and leaves of the higher gymnosperm yew (Taxus brevifolia). Among the more than 200 taxane compounds that have been isolated so far, many have been proven to have cytotoxicity and antitumor activity. [0003] Paclitaxel and docetaxel can stabilize cell microtubules and prevent depolymerization of cell microtubules, thereby preventing cell division and inhibiting the growth of cancer cells. Therefore, they have the effect of treating cancer and have been widely used clinically. [0004] Paclitaxel is considered to be the most important discovery in the field of natural ...

Claims

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Application Information

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IPC IPC(8): C07D305/14A61K31/337A61P35/00
Inventor 季晓铭姚勇李严卓忠浩郑云满
Owner SHANGHAI TECHWELL BIOPHARMACEUTICALS CO LTD
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