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A kind of purification method of belistat

The technology of a belinostat and purification method is applied in the field of purification of the antineoplastic drug belinostat, which can solve the problems of high purification yield and inability to obtain the raw material drug of belinostat, and achieve simple and convenient operation Effect

Active Publication Date: 2021-11-09
深圳万乐药业有限公司
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The invention provides a method for purifying the raw material drug of belistat. The method only uses one crystallization operation, and the operation is simple and convenient, which can solve the defect that the raw material drug of belistat in the form of a pure white solid cannot be obtained in the prior art. And the purification yield of the product is high, and the purity of the product can reach more than 99%

Method used

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  • A kind of purification method of belistat
  • A kind of purification method of belistat

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Experimental program
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Effect test

Embodiment 1

[0018] The synthesis of embodiment 1 Belinostat

[0019] The synthesis of Belinostat of the present invention adopts the following synthetic route:

[0020]

[0021] For the specific operation method of crude product synthesis, see Chinese patent CN104478769A, the obtained crude belistat is brownish yellow, and the product purity is 96.8%.

Embodiment 2

[0022] The purification of embodiment 2 Belinostat

[0023] Dissolve 30g of the crude belistat in 180ml of methanol until clear. Take a 2000ml reaction bottle, add 1500ml of water and 75ml of ethyl acetate and stir evenly, add the methanol solution of the crude belistat into the reaction bottle and stir at room temperature for 20min. Then, 27.3 g of white solid was obtained by filtration, with a yield of 91% and a purity of 99.2%.

Embodiment 3

[0024] The purification of embodiment 3 Belinostat

[0025] Dissolve 50g of the crude belistat in 450ml of methanol until clear, take a 5000ml reaction bottle, add 2000ml of water and 100ml of ethyl acetate and stir evenly. Add the methanol solution of the crude belistat into the reaction bottle and stir at room temperature for 20min. Then it was filtered to obtain 43.2 g of white solid. The yield was 86.5%, and the purity was 99.0%.

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Abstract

The invention provides a method for purifying the raw material drug of belistat, which uses methanol as a dissolving solvent and water-ethyl acetate as a crystallization solvent to carry out recrystallization, and can purify the raw material drug of belinostat to obtain The pure white product solves the defect that the prior art cannot be purified to obtain a pure white product, and the method is simple to operate, does not need to use activated carbon for decolorization, does not need multiple crystallization purification, is easy to operate, and is suitable for industrial production.

Description

technical field [0001] The invention relates to the field of medicinal chemistry, in particular to a purification method of the antineoplastic drug belistat. Background technique [0002] Belinostat (PXD101) is a histone deacetylase inhibitor (HDACi) developed by Topotarget AS, Denmark. Overexpression or abnormal regulation of histone deacetylase (HDAC) will lead to excessive deacetylation of histones, remodeling chromatin into a configuration that inhibits transcription, causing a decrease in the expression of corresponding genes, leading to cancer. Inhibition of HDACs is considered a promising anticancer drug target. Belinostat can directly act on the abnormal expression of genes, thereby inhibiting and correcting the excessive proliferation and abnormal differentiation of tumor cells. For common drug resistance problems, it can also be used in combination with drugs with other mechanisms of action. Belinostat can effectively inhibit the proliferation of solid tumor cell...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07C311/21C07C303/44
CPCC07C303/44C07C311/21
Inventor 李昌希张莉孙鹏杰于玉根
Owner 深圳万乐药业有限公司