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Purifying method for carfilzomib

A technology of carfilzomib and purification method, which is applied in the preparation methods of peptides, chemical instruments and methods, organic chemistry, etc., can solve the problems of poor purification effect and difficult purification.

Active Publication Date: 2016-10-05
CHIA TAI TIANQING PHARMA GRP CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] Due to the similar structure of the isomer impurity and carfilzomib, the purification is difficult, and the purification effect of conventional methods is not good

Method used

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  • Purifying method for carfilzomib
  • Purifying method for carfilzomib
  • Purifying method for carfilzomib

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] The preparation of embodiment 1 carfilzomib maleate

[0042] Dissolve 200g of carfilzomib (purity 99.0%) in 4L of tetrahydrofuran, add 34g of maleic acid, stir to dissolve, add 1L of acetonitrile, stir for 2h, filter, wash with acetonitrile, and dry under reduced pressure to obtain 206g of carfilzomib maleic acid Salt (purity 99.6%), yield 89%.

Embodiment 2

[0043] The preparation of embodiment 2 carfilzomib maleate

[0044] 20g carfilzomib (purity 99.0%) was dissolved in 400mL tetrahydrofuran, added 3.6g maleic acid, stirred at room temperature for 2h, filtered, washed with tetrahydrofuran, and dried under reduced pressure to obtain 19.8g carfilzomib maleate (purity 99.7%) %), yield 85%.

Embodiment 3

[0045] The preparation of embodiment 3 carfilzomib maleate

[0046] 20g carfilzomib (purity 98.5%) was added in 400mL acetone, heated and dissolved, added 3.4g maleic acid, stirred at room temperature for 2h, filtered, washed with acetone, and dried under reduced pressure to obtain 19.5g carfilzomib maleate ( Purity 99.5%), yield 84%.

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Abstract

The invention specifically relates to a purifying method for carfilzomib, belonging to the field of pharmaceutical chemicals. According to the method, maleic acid is added in the preparation process of carfilzomib to prepare carfilzomib maleate, so isomer impurities are obviously reduced and purity is substantially improved; and then maleate is subjected to dissociation so as to obtain high-yield high-purity carfilzomib. The method is simple in preparation, easy to operate and especially suitable for industrial production.

Description

technical field [0001] The invention belongs to the field of medicine and chemical industry, and in particular relates to a method for purifying carfilzomib. Background technique [0002] Carfilzomib (Carfilzomib, formula I), chemical name (2S)-N-((S)-1-((S)-4-methyl-1-((R)-2-methylepoxy Ethane-2-yl)-1-oxopentan-2-ylcarbamoyl)-2-phenethyl)-2-((S)-2-(2-morpholinoacetamido)4 -Phenylbutyramide)-4-methylpentanamide, is a second generation protease inhibitor. Carfilzomib was launched in the United States in September 2012. The marketed product is freeze-dried powder for intravenous injection, with the trade name Kyprolis. Multiple myeloma patients with disease progression within 60 days of treatment. [0003] [0004] Example 6 of WO2005105827 discloses the synthesis of carfilzomib, and documents such as CN103360348A, CN103641890A and CN104086624A disclose the preparation method of carfilzomib. [0005] Carfilzomib is a polypeptide analog, and the structure of the isomer i...

Claims

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Application Information

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IPC IPC(8): C07K7/06C07K1/30
Inventor 程兴栋张爱明夏春光张喜全刘国瑞姜奇朱雪焱
Owner CHIA TAI TIANQING PHARMA GRP CO LTD
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