A kind of refining method of pitavastatin tert-butyl ester

A technology of pitavastatin tert-butyl ester and a refining method, applied in the directions of organic chemistry, organic chemistry, etc., can solve problems such as inability to remove, influence, etc., and achieve the effects of low uncontrollability, good refining effect and high yield
CN108997212BActive Publication Date: 2021-03-09ZHEJIANG JINGXIN PHARMA
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
ZHEJIANG JINGXIN PHARMA
Publication Date
2021-03-09

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Abstract

The invention discloses a refining method of pitavastatin tert-butyl ester, which comprises the following steps: cooling and crystallizing a mixed solvent in which pitavastatin tert-butyl ester raw materials are dissolved, filtering, and drying; wherein, the mixed solvent It is a mixture of methyl tert-butyl ether and non-polar organic solvent; the non-polar organic solvent is n-hexane, n-heptane, cyclohexane, n-pentane, cyclopentane, octane or isooctane. According to the refining method of the present invention, the isomer content in the obtained pitavastatin tert-butyl ester is low, and the refining effect is good. Epimer impurity 1, epimer impurity 2 and enantiomer impurity The contents are all below 0.05%. Moreover, the refining method of the present invention has high yield, low uncontrollability, simple operation, is suitable for large-scale industrial production, and can prepare high-purity pitavastatin calcium.
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Description

technical field

[0001] The invention relates to a refining method of pitavastatin tert-butyl ester. Background technique

[0002] Coronary heart disease is a common and frequently-occurring disease that threatens human health and life. Hypercholesterolemia characterized by elevated low-density lipoprotein (LDL) is one of the main risk factors for coronary heart disease. Commonly used blood lipid-lowering drugs such as niacin, resins or fibrates have unsatisfactory curative effects, and the drugs with the best lipid-lowering effect are known as statins (statins). The common mechanism of action of statins is that they all belong to 3-hydroxy-3-methyl-glutaryl coenzyme A (HMG-CoA) reductase inhibitors. At present, there are mainly six kinds widely used in the world: lovastatin (lovastatin) ), pravastatin, simvastatin, cerivastatin, fluvastatin and atorvastatin. Pitavastatin Calcium, developed by Kowa Company, is called "Superstatin" because of its good cholesterol-lowering ef...

Claims

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