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Lovastatin purification method combining auxiliary magnetic crystallization

A technology of lovastatin and a purification method, which is applied in the field of separation and purification of lovastatin, and can solve the problems of low product purity and the like

Active Publication Date: 2015-06-24
NEW FOUNDER HLDG DEV LLC +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The crude product is obtained after centrifugal drying, and the obtained product has low purity

Method used

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  • Lovastatin purification method combining auxiliary magnetic crystallization

Examples

Experimental program
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Effect test

Embodiment 1

[0019] 80g of crude lovastatin was dissolved in 250ml of ethanol, 1.4g of activated carbon was added, and the volume was fixed to 280ml. It was divided into two parts. Gradually cool until a large amount of crystals are precipitated, stop the magnetic assistance, continue cooling to 10°C, filter with suction, and dry in vacuum to obtain the finished product.

Embodiment 2

[0021] 80g of crude lovastatin was dissolved in 200ml of ethanol, 1.4g of activated carbon was added, and the volume was fixed to 230ml. It was divided into two parts. One part was crystallized on standing; Gradually cool until a large amount of crystals are precipitated, stop the magnetic assistance, continue to cool to 15°C, filter with suction, and dry in vacuum to obtain the finished product.

Embodiment 3

[0023] Dissolve 80g of lovastatin crude product in 300ml of ethanol, add 1.4g of activated carbon, heat filter, set volume to 320ml, divide into two parts, one part is left to crystallize; the other part is crystallized by 0.6T magnetic field during cooling crystallization, Gradually cool until a large amount of crystals are precipitated, stop the magnetic assistance, continue cooling to 5°C, filter with suction, and dry in vacuum to obtain the finished product.

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Abstract

The invention discloses a lovastatin purification method combining auxiliary magnetic crystallization, which comprises the following steps: dissolving a lovastatin crude product in organic solvent, and then gradually cooling the lovastatin solution; and applying a magnetic field to the solution until crystals are precipitated, and separating and drying the crystals to obtain a lovastatin product. In the crystallization process, the ordered arrangement of lovastatin molecules is increased through auxiliary magnetic treatment, thereby increasing the quality and quantity of high-purity crystal nuclei, improving the crystallization conditions, obtaining the crystals which are high in purity and easy to separate and enhancing the product quality.

Description

technical field [0001] The invention relates to a method for separating and purifying lovastatin, in particular to a method for further separating and purifying crude lovastatin extracted from fermented liquid of Aspergillus terreus through crystallization. Background technique [0002] A new type of blood lipid-lowering drug lovastatin (LOVASTATIN), the chemical name is: (S)-2-methylbutyric acid-(1S, 3S, 7S, 8S, 8aR)-1, 2, 3, 7, 8, 8a - Hexahydro-3,7-dimethyl-8-{2-[(2R,4R)-4-hydroxy-6-oxo-2-tetrahydropyranyl]-ethyl}-1-naphthyl ester; Molecular formula is C 24 h 36 o 5 , the molecular weight is 404.55, and the structure is as follows: [0003] [0004] Merck's lovastatin (lovastatin, Mevacor) immediately attracted the attention of the medical community after it was approved by the FDA in 1987. Lovastatin has successfully created a new stage of lipid-lowering drugs. The drug inhibits the activity of the rate-limiting enzyme hydroxymethylglutaryl coenzyme A reductase ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D309/30
Inventor 彭平郭萍张洪兰王先文
Owner NEW FOUNDER HLDG DEV LLC
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