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Preparation method of amorphous cabazitaxel

An amorphous technology of cabazitaxel, which is applied in the field of preparation of taxane compounds, can solve the problem that the residual amount of solvent is difficult to reach a high standard, and achieve the effect of good and stable physical and chemical state and easy operation

Active Publication Date: 2014-02-26
SHIJIANGZHUANG ZHIHENG PHARMACY TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

After testing and research by the inventors, it is found that the residual solvent content of cabazitaxel prepared by the existing method is difficult to reach a high standard regardless of whether it is in a crystalline form or an amorphous form.

Method used

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  • Preparation method of amorphous cabazitaxel
  • Preparation method of amorphous cabazitaxel
  • Preparation method of amorphous cabazitaxel

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] The preparation of embodiment 1 amorphous cabazitaxel

[0037] Dissolve 1 g of cabazitaxel in 10 ml of methanol, place it in a watch glass, volatilize under normal pressure at 30°C, and dry at elevated temperature at 40°C to obtain 0.9 g of amorphous cabazitaxel. Methanol solvent residue: 0% (limit 0.3%)

Embodiment 2

[0038] The preparation of embodiment 2 amorphous cabazitaxel

[0039] Dissolve 1 g of cabazitaxel in 10 ml of dichloromethane, put it in a watch glass, volatilize under normal pressure at 30 ° C, and dry at 40 ° C to obtain 0.9 g of amorphous cabazitaxel. Dichloromethane solvent residue: 0.03% (limit 0.06%)

Embodiment 3

[0040] The preparation of embodiment 3 amorphous cabazitaxel

[0041] Dissolve 1 g of cabazitaxel in 10 ml of acetone, put it in a watch glass, dry it under reduced pressure at 30°C, and dry at 40°C to obtain 0.9 g of amorphous cabazitaxel. Acetone solvent residue: 0.26% (limit 0.5%)

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Abstract

The invention relates to a preparation method of amorphous cabazitaxel. The method comprises the steps of dissolving cabazitaxel in an organic solvent, putting in an appropriate vessel, volatilizing the solvent at normal pressure or pumping the solvent under reduced pressure, and drying to obtain the amorphous cabazitaxel. The cabazitaxel provided by the invention is good in appearance and stability and low in solvent residue; the preparation method is simple in operation and easy in industrialization.

Description

technical field [0001] The invention relates to a preparation method of taxane compounds, in particular to an amorphous cabazitaxel and a preparation method thereof. Background technique [0002] Cabazitaxel is a chemical semi-synthetic taxane compound, which has a similar structure to the natural anticancer active ingredient paclitaxel. It was developed by the French Sanofi-Aventis pharmaceutical company and was approved by the US FDA in June 2010. It is used for Second-line therapy against prostate cancer. Its chemical name is 4-acetoxy-2α-benzoyloxy-5β,20-epoxy-1-hydroxy-7β,10β-dimethoxy-9-oxotaxane-11-ene- 13α-yl(2R,3S)-3-tert-butoxycarbonylamino-2-hydroxy-3-phenylpropionate. [0003] The structural formula is as follows: [0004] [0005] Cabazitaxel is polymorphic. [0006] Chinese patent CN200480026128.X characterizes the crystal form A of cabazitaxel, namely acetone solvate. This crystal form is currently the only pharmaceutical crystal form approved by the F...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D305/14
CPCC07D305/14
Inventor 赵军旭刘子龙王璐
Owner SHIJIANGZHUANG ZHIHENG PHARMACY TECH CO LTD
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