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Pitavastatin (III) refining method

A technique of refining pitavastatin, which is applied in the field of drug synthesis, can solve the problems of low yield, difficult purification, and unsuitability for large-scale industrial production, and achieve the effects of increasing yield, reducing solvent consumption, and reducing heating time

Active Publication Date: 2018-08-10
HUBEI JINGJIANGYUAN PHARMA
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0009]The main disadvantage of this process is that the process uses column chromatography to purify the intermediates, which is not suitable for industrialized large-scale production
In addition, due to the difficulty of purification, the yield is low, which is also a difficult problem in industrial production.

Method used

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  • Pitavastatin (III) refining method

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Embodiment 1

[0036] The refining method of pitavastatin with high optical purity, which is suitable for industrial production, has few impurities and high yield, is carried out according to the following steps:

[0037] Step 1: Prepare a mixed solvent of water, DMF and methyl isobutyl ketone, the weight ratio of water, DMF and methyl isobutyl ketone is 2:10:180.

[0038] Step 2: The crude product of pitavastatin (Ⅲ) (8.4kg, purity: 78.9%, epimer: 0.72%, Z-isomer: 13.5%, its HPLC figure is shown in Figure 4 shown) was added to the mixed solvent to dissolve and mechanically stirred. The weight of the mixed solvent was 21kg, which was 2.5 times the weight of the crude product of pitavastatin (Ⅲ). D-(+)-α-methylbenzylamine (2.5kg), continue to maintain stirring, solids begin to precipitate, and the suspension is maintained at 20-30°C and stirred for 2 hours;

[0039] Step 3: filter the suspension, drain as far as possible to no drip, then wash the filter cake with a small amount of mixed sol...

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Abstract

The invention belongs to the field of drug synthesis, and particularly relates to a pitavastatin (III) refining method. According to the present invention, the pitavastatin crude product (III) and D-(+)-alpha-methylbenzylamine salt form the salt in the mixed solvent so as to maximally remove the impurities; the refining is performed with the mixed solvent, wherein the solvent used for beating is less so as to increase the yield, reduce the solvent consumption and reduce the cost; and pitavastatin (III) is unstable, wherein the solvent is pre-heated, and the beating temperature is lower than the boiling point of the organic solvent in the mixed solvent so as to shorten the heating time of the product and avoid the generation of the impurities.

Description

technical field [0001] The invention belongs to the field of medicine synthesis, and in particular relates to a refining method of pitavastatin (III). Background technique [0002] Pitavastatin Calcium is the first fully synthetic HMG-CoA reductase inhibitor developed by Nissan Chemical Co., Ltd. and Kowa Co., Ltd. It was registered in Japan in November 1999, and was first approved for marketing in Japan in July 2003 . Foreign countries are known as "super statins" for their powerful lipid-lowering effects shown in clinical trials. According to the results of the existing clinical trials and the comparison with similar foreign products already on the market, its lipid-lowering effect is very good, and it is the most powerful lipid-lowering drug so far. [0003] Many domestic and foreign literatures have reported the synthesis process of pitavastatin calcium. Based on the comprehensive literature, the synthesis process of pitavastatin calcium can be divided into two parts: ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D215/14
CPCC07D215/14C07B2200/07Y02P20/55
Inventor 王力王诗宏王登科付伟程宋新莉李习武
Owner HUBEI JINGJIANGYUAN PHARMA
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