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Lovastatin purification method

A lovastatin and organic solvent technology, applied in the field of further separation and purification of crude lovastatin, can solve the problem of low product purity

Active Publication Date: 2015-04-29
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

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] 60g crude lovastatin is dissolved in 200ml ethanol, add 1.2g activated carbon, hot filter, constant volume 200ml, divided into two parts, gradually reduce the temperature of the solution, one part is allowed to stand for crystallization; the other part is observed when the solution is crystallized , Turn on 20W microwave assist. Continue to gradually cool to 10°C, a large amount of crystals are precipitated, stop microwave assistance, suction filtration, and vacuum drying to obtain a finished product.

Embodiment 2

[0021] 60g crude lovastatin is dissolved in 160ml ethanol, add 1.2g activated carbon, hot filter, constant volume 160ml, divided into two parts, gradually reduce the temperature of the solution, one part is allowed to stand for crystallization; the other part is observed when the solution is crystallized , Turn on 40w microwave assist. Continue to gradually cool to 15°C, a large amount of crystals will precipitate, stop microwave assistance, suction filtration, vacuum drying, and get the finished product.

Embodiment 3

[0023] 60g crude lovastatin is dissolved in 240ml ethanol, add 1.2g activated carbon, hot filter, constant volume 240ml, divided into two parts, gradually reduce the temperature of the solution, one part is allowed to stand for crystallization; the other part is observed when the solution is crystallized , Turn on 60w microwave assist. Continue to gradually cool to 5°C, a large amount of crystals will precipitate out, stop microwave assistance, suction filtration, vacuum drying, and get the finished product.

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Abstract

The invention discloses a lovastatin purification method which comprises the following steps: dissolving a lovastatin crude product in organic solvent, and gradually cooling; when observing that the crystallization phenomenon exists in the solution, performing microwave treatment on the solution, and further cooling to crystallize; and after a large amount of crystals are precipitated, stopping microwave treatment, and separating and drying the crystals to obtain a lovastatin product. In the crystallization process, fragile grains are dissolved through the auxiliary microwave treatment, so that crystal nuclei having high purity are left to become the variety, thereby 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 separation and purification of lovastatin, in particular to a method for further separation and purification of crude lovastatin extracted from the fermentation broth of Aspergillus terreus. Background technique [0002] Lovastatin (LOVASTATIN), chemical name: (S)-2-methylbutanoic acid-(1S,3S,7S,8S,8aR)-1,2,3,7,8,8a-hexahydro-3 , 7-dimethyl-8-{2-[(2R, 4R)-4-hydroxy-6oxo-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] In 1987, after Merck's lipid-lowering drug lovastatin (Mevacor) was approved by the FDA for marketing, it immediately attracted the attention of the medical community. The success of this drug created a new stage of lipid-lowering drugs. The drug inhibits the activity of the rate-limiting enzyme hydroxymethylglutaryl coenzyme A reductase (HMG-CoA reductase) in the process of cholesterol synth...

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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