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Cabazitaxel isopropyl etherate and its crystallization

A technology of cabazitaxel and etherate, applied in the field of medicinal chemistry, can solve the problems of high industrialization cost, insufficient stability, and complicated preparation methods, and achieve the effects of good stability, excellent physical and chemical properties, and simple preparation process

Active Publication Date: 2016-01-20
SHANGHAI INST OF PHARMA IND CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] However, the applicant found that the cabazitaxel and its solvates disclosed in the prior art are not stable enough, and the preparation method is complicated and the industrialization cost is high

Method used

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  • Cabazitaxel isopropyl etherate and its crystallization
  • Cabazitaxel isopropyl etherate and its crystallization
  • Cabazitaxel isopropyl etherate and its crystallization

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Dissolve cabazitaxel (2 g) in 20 ml of acetic acid, add 60 ml of isopropyl ether dropwise with stirring at room temperature, stir for 2 hours, filter with suction, wash the solid with isopropyl ether, and dry it in vacuum (55°C) for about 3 hours to obtain 1.5 g of white solid . The mass percent content of isopropyl ether in the product was determined by gas chromatography to be 9.65%.

Embodiment 2

[0041] Dissolve cabazitaxel (2 g) in 10 ml of acetic acid, add 30 ml of isopropyl ether dropwise with stirring at room temperature, stir for 2 hours, filter with suction, wash the solid with isopropyl ether, and dry it in vacuum (55°C) for about 3 hours to obtain 1.55 g of white solid . The mass percent content of isopropyl ether in the product was determined by gas chromatography to be 9.24%.

Embodiment 3

[0043] Dissolve cabazitaxel (2 g) in 30 ml of acetic acid, add 90 ml of isopropyl ether dropwise with stirring at room temperature, stir for 2 hours, filter with suction, wash the solid with isopropyl ether, and dry it in vacuum (55°C) for about 3 hours to obtain 1.51 g of white solid . The mass percent content of isopropyl ether in the product was determined by gas chromatography to be 9.68%.

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Abstract

The invention relates to a cabazitaxel isopropyl ether compound and a crystal thereof, and specifically, relates to the cabazitaxel isopropyl ether compound and the crystal thereof, methods for preparing the cabazitaxel isopropyl ether compound and the crystal thereof, pharmaceutical compositions containing the cabazitaxel isopropyl ether compound and the crystal thereof, and an application of the cabazitaxel isopropyl ether compound and the crystal thereof and the pharmaceutical compositions in preparing antitumor drugs. The cabazitaxel isopropyl ether compound and the crystal thereof have the advantages of being excellent in physicochemical properties, good in stability, simple in preparation technology, more suitable for industrialized scale preparation and the like.

Description

technical field [0001] The invention relates to the field of medicinal chemistry, in particular to the isopropyl ether compound of the anti-malignant tumor compound cabazitaxel, and also relates to its crystallization. technical background [0002] Taxane compounds have strong anti-tumor activity, and such compounds are currently on the market, such as paclitaxel, docetaxel and cabazitaxel, etc., which have good inhibitory activity on various solid tumor cells. Among them, cabazitaxel, namely 4-acetoxy-2α-benzoyloxy-5β, 20-epoxy-1-hydroxy-7β, 10β-dimethoxy-9-oxotaxane-11 -en-13α-yl (2R,3S)-3-tert-butoxycarbonylamino-2-hydroxyl-3-phenylpropionate (structure shown in the following formula), developed and marketed by Sanofi, France Taxane anti-tumor drugs, the drug has better curative effect on patients with advanced prostate cancer. Compared with other anti-tumor drugs, this drug can significantly improve the vitality of patients with advanced prostate cancer and prolong the ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D305/14A61K31/337A61P35/00
CPCC07D305/14
Inventor 袁哲东杨玉雷朱雪焱程兴栋张爱明孙键
Owner SHANGHAI INST OF PHARMA IND CO LTD