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Technique for preparing fluvastatin sodium crystal system

A technology of fluvastatin sodium and fluvastatin, which is applied in the technical field of preparing fluvastatin sodium crystal form, can solve the problems of large amount of raw materials, insufficient disclosure of instructions, difficulty in fluvastatin sodium type B crystal, etc., and achieves improvement The effect of utilization rate, short time and simple operation

Inactive Publication Date: 2008-08-27
SHENZHEN SALUBRIS PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although this patent discloses the process of preparing fluvastatin sodium crystal form B by reacting fluvastatin acid, ester or salt with sodium salt compound, the process does not disclose the specific steps and experimental data required to implement the scheme, nor does it disclose Any embodiment is supported, so its specification disclosure is not sufficient enough to enable those skilled in the art to implement the technical solution
In addition, in actual operation, the mixed solution of methanol or ethanol and water is used as the solvent system, because the solubility of the solvent system to fluvastatin sodium is very large, so not only the amount of raw materials input is large, but also the actual precipitation of fluvastatin sodium Type B crystals are also difficult

Method used

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  • Technique for preparing fluvastatin sodium crystal system
  • Technique for preparing fluvastatin sodium crystal system
  • Technique for preparing fluvastatin sodium crystal system

Examples

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Effect test

Embodiment 1

[0046] Dissolve 100g of fluvastatin methyl ester in 1800mL of acetone, add 30mL of water, then add 10g of sodium hydroxide, stir, slowly raise the temperature to 60°C and react for 4 hours, then cool down to room temperature naturally. The solid was obtained by filtration, washed twice with acetone / water (9 / 0.8v:v), and dried under vacuum at 50°C to obtain 92g of off-white solid-fluvastatin sodium type B. (HPLC: 99.8%).

Embodiment 2

[0048] Heat and dissolve 10 g of fluvastatin methyl ester with 300 mL of methyl isobutyl ketone, filter, add 3 mL of water, then add 0.95 g of sodium hydroxide, stir, and slowly raise the temperature to 65°C for 4 hours of reaction. The solid was obtained by filtration, washed twice with acetone / water (9 / 0.8v:v), and vacuum-dried at 50°C to obtain 8.8g of off-white solid-fluvastatin sodium type B. (HPLC: 99.0%).

Embodiment 3

[0050] Dissolve 5 g of fluvastatin ethyl ester in 100 mL of 3-pentanone, filter, add 2 mL of water, and then add 0.40 g of sodium hydroxide, stir, and slowly raise the temperature to 65°C for 4 hours. The solid was obtained by filtration, washed twice with acetone / water (9 / 0.8v:v), and dried under vacuum at 50°C to obtain 4.2 g of off-white solid-fluvastatin sodium type B. (HPLC: 99.4%).

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Abstract

The invention provides a preparation method of fluvastatin sodium B type crystal. The invention uses the mixture solvent of organic solvent and water, which has suitable polarity and different solubilities on fluvastatin ester and fluvastatin sodium, therefore the mixture solvent can be used as the reaction system of fluvastatin low class alkyl ester and alkali compound of sodium and can be used as the crystallization system of fluvastatin sodium, to directly precipitate crystal after complete reaction without adding sediment solvent. The whole operation is simple and short, and only needs several hours (5-8h) to prepare the product whose purity is at least 99% and yield is at least 91%. The invention is suitable for industrial production.

Description

Technical field: [0001] The invention relates to a preparation process of compound crystal form, in particular to a preparation process of fluvastatin sodium crystal form B. Background technique: [0002] Fluvastatin (Fluvastatin) is a second-generation blood lipid-lowering product, successfully developed by the Swiss company Sandoz, and produced by Novartis. [0003] The fluvastatin compound patent was applied for WO8402131 in November 1983, and the application for the crystal form patent began in June 1997. The patent number is US6124340, which is believed to be produced by lyophilization in Examples 6 (b) and 8 of US Patent US4739073 Solid fluvastatin sodium is a mixture of crystalline form (referred to as Form A) and amorphous material, while another crystal form B with low hygroscopicity and light resistance is disclosed. Since then, the crystal forms have been extensively studied. So far, nearly 100 crystal forms of fluvastatin have been discovered, and only patents W...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D209/24
Inventor 付鑫祥李孝仁黄群辉
Owner SHENZHEN SALUBRIS PHARMA CO LTD
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