Fluvastatin sodium compound and preparation method thereof

A technology of fluvastatin sodium and its compound, which is applied in the field of fluvastatin sodium compound and its preparation method, can solve the problems of low purity of fluvastatin sodium, achieve easy control and industrial production, improve clinical adverse reactions, and improve product quality Effect

Inactive Publication Date: 2012-02-15
HAINAN MEIDA PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0015] In order to overcome the defects of the above-mentioned prior art, especially the defect of low purity of fluvastatin sodium prepared by the prior art, the invention provides a method for refining fluvastatin sodium compound

Method used

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  • Fluvastatin sodium compound and preparation method thereof
  • Fluvastatin sodium compound and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0059] Get 10g of fluvastatin sodium crude product with a purity of 86.3% prepared according to route 1, dissolve it in 200ml of water, add 0.2g of gac, stir, absorb for 10 minutes, filter with suction, and collect the filtrate.

[0060] 1 g of sodium methoxide was added to the above filtrate and treated at room temperature for 1 hour, the precipitated precipitate was filtered off, and the filtrate was collected.

[0061] Add 100ml of acetone to the above-mentioned filtrate, during this process crystals are slowly precipitated, placed at room temperature for 5 hours, the crystallization is complete, washed with 10ml of purified water, and dried to obtain 8.4g of refined fluvastatin sodium with a purity of 98.6% and a yield of 95.6% .

[0062] 1 H-NMR (CD 3 OD): δ1.52~1.48(1H, m), 1.60~1.71(7H, m), 2.35~2.20(2H, m), 3.99~3.94(1H, m), 4.38~4.34(1H, m), 4.92(1H, hept, J=6.8Hz), 5.73(1H, dd, J=16.0, 6.0Hz), 6.67(1H, dd, J=16.2, 1.2Hz), 6.98(1H, t, J=7.2Hz ), 7.12~7.08 (3H, m),...

Embodiment 2

[0068] Get 10g of fluvastatin sodium crude product with a purity of 88.9% prepared according to route 2, dissolve it in 1000ml of water, add 3g of gac, stir, absorb for 30 minutes, filter with suction, and collect the filtrate.

[0069] Add 2 g of sodium ethylate to the above filtrate and treat at room temperature for 1 hour, filter the precipitated precipitate, and collect the filtrate.

[0070] Add 800ml of acetone to the above-mentioned filtrate, during this process crystals are slowly precipitated, placed at room temperature for 12 hours, the crystallization is complete, washed with 20ml of purified water, and dried at 50°C to obtain 8.5g of refined fluvastatin sodium with a purity of 98.8%. 94.5%. mp196°C.

Embodiment 3

[0076] Get 10g of fluvastatin sodium crude product with a purity of 84.1% prepared according to route 3, dissolve it in 500ml of water, add 1g of activated carbon, stir, absorb for 20 minutes, filter with suction, and collect the filtrate.

[0077] Add 1 g of sodium ethylate to the above filtrate and treat at room temperature for 1 hour, filter out the precipitated precipitate, and collect the filtrate.

[0078] Add 500ml of acetone to the above filtrate, during this process crystals slowly precipitate out, place at room temperature for 12 hours, the crystallization is complete, wash with purified water, and dry at 50°C to obtain 8.2g of refined fluvastatin sodium with a purity of 98.8% and a yield of 96.3 %. mp196℃

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Abstract

The invention discloses a fluvastatin sodium compound and a preparation method thereof. The preparation method comprises the following steps of: 1, dissolving a fluvastatin sodium raw material in water, adding a proper amount of active carbon, stirring for adsorption, performing suction filtration, and collecting filtrate to obtain the primarily purified fluvastatin sodium-containing aqueous solution; 2, treating the aqueous solution by adding alkali metal or alkaline-earth metal alkoxides, and filtering to obtain filtrate, namely the secondarily purified fluvastatin sodium-containing aqueous solution; and 3, adding a poor solvent of fluvastatin sodium into the solution, controlling temperature for recrystallization, centrifugally washing, and drying to obtain the triply purified fluvastatin sodium. By the method, the quality of the preparation product is improved, the toxic and side effects of the fluvastatin sodium in preparation of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase inhibitors are reduced, and the method is particularly suitable for industrial production.

Description

technical field [0001] The invention relates to a fluvastatin sodium compound and a preparation method thereof, belonging to the technical field of medicine. Background technique [0002] Fluvastatin sodium (Fluvastatin sodium), the chemical name is 3R * , 5S * -(E)]-(±)-7-[3-(4-fluorophenyl)-1-isopropyl-1H-indol-2-yl]-3,5-dihydroxy-6-heptene Sodium Acid, Molecular Formula C 24 h 25 FNNaO 4 , the structural formula is: [0003] [0004] Fluvastatin sodium, developed by Sandoz AG in Sweden, was first launched in the United States in 1993. It is the first competitive inhibitor of HMG-CoA reductase obtained through total synthesis. Fluvastatin sodium has a significant effect on reducing serum total cholesterol, low-density lipoprotein (LDL) and triglyceride levels. [0005] Domestic and foreign literature reports that the synthetic routes of fluvastatin sodium mainly include: route 1, fluorobenzene and chloroacetyl chloride carry out F-C acylation to obtain 4-chloroac...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D209/24A61K31/405A61P3/06
Inventor 廖爱国
Owner HAINAN MEIDA PHARMA
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