Isolation of taxanes

一种紫杉烷类、化合物的技术，应用在有机化学等方向，能够解决成本高、增加成本、溶剂不能被容易地回收等问题，达到降低生产成本、降低开销的效果

Inactive Publication Date: 2004-03-31
拉胡·塞吉
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Since in this method, the solvent used in each step cannot be easily recovered for subsequent separation, this greatly increases the cost of production
[0012] Therefore, the methods for isolating and purifying paclitaxel from raw materials or crude extracts in the prior art are limited or have the characteristics of complicated process, high cost and small scale.

Method used

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  • Isolation of taxanes
  • Isolation of taxanes
  • Isolation of taxanes

Examples

Experimental program
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Embodiment

[0035] All chemicals used were commercially available and were tested analytically before use. All glass chromatographic columns and silica gel were purchased from China Far East Pharmaceutical Instrument Co., Ltd., and industrial solvents were purchased from Stanchen Company in Canada. The standard products used in HPLC, such as paclitaxel, cephalomannine, 9-dihydro-13- Acetyl-baccatin III was purchased from Hauser Company of the United States, fluorescent silica gel TLC thin plate was purchased from Waters Company of the United States, and a Dionex 500 HPLC system was used to analyze the components in the method of the present invention.

[0036] The crude extract (0.5 kg) derived from the needles of Taxus canadensis was dissolved in 4 L of ethyl acetate. The solution was loaded into an industrial-grade glass chromatographic column (15 cm×100 cm), which had previously been filled with silica gel powder (1×250 mesh) for about 70% of the column height. Elution was performed u...

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Abstract

An improved method for the isolation of taxanes of high priority from the crude extract of naturally occurring Taxus canadensis which comprises the steps of: a) filtering the crude extract by liquid column chromatography b) enriching the taxanes obtained from step a) by precipitation and crystalization; c) separating the taxanes obrained from step a) by liquid column chromatography and d) desolving the separate taxanes in a polar organic solvent mixture comprising an alcohol and a non-alcohol solvent, which solution is then subjected to further separation by liquid column chromatography and isolaring substantially pure paclitaxel from cephalomannine; and all solvent mixtures used may be collected, purified and recycled without seperation.

Description

technical field [0001] The present invention relates to a method for isolating and producing taxane compounds from the crude extract of Taxus canadensis distributed in the eastern provinces of Canada. More specifically, the present invention relates to a high yield chromatographic separation of substantially pure paclitaxel, cephalomannine, and 13-acetyl-9-dihydro-baccatin III (baccatin The method of baccatin III). Background of the invention [0002] Paclitaxel is an important active pharmaceutical ingredient used in metastatic cancer chemotherapy. The antitumor activity of paclitaxel lies in its interference with mitosis. Paclitaxel has been approved by the US Federal Drug Administration (FDA) and the Health Protection Branch of Health Canada for the treatment of ovarian cancer. Results from ongoing clinical trials for the treatment of other cancers, such as breast, lung and colon cancer, are also promising. [0003] Paclitaxel, a natural product originally isolated fr...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D305/14
CPCC07D305/14
Inventor 拉胡·塞吉
Owner 拉胡·塞吉
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