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Method for preparing amlodipine benzenesulfonate

A kind of technology of amlodipine besylate and amlodipine, which is applied in the field of preparation of amlodipine besylate, can solve the problems of increasing reaction steps, increasing costs, unfavorable product quality control, etc., and achieves simple operation process and high yield High, easy-to-control product quality

Active Publication Date: 2006-10-25
SUZHOU DAWNRAYS PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although this method has a higher yield than method one, it needs to first salt amlodipine during its preparation, and then react with besylate, which increases the reaction steps and increases the cost for industrial production
This method is owing to utilize metathesis reaction to prepare amlodipine besylate in addition, so raw material amlodipine salt is difficult to completely eliminate in the obtained amlodipine besylate, unfavorable to the quality control of product

Method used

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  • Method for preparing amlodipine benzenesulfonate

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0016] Mix 99% isopropyl acetate and 99% isopropanol in a volume ratio of 5:1 to form a mixed solvent.

[0017] Dissolve 10g of amlodipine base (24.46mmol) in 80ml of the aforementioned mixed solvent, maintain the temperature at 0-5°C, and slowly add dropwise 4g (25.3mmol) of anhydrous benzenesulfonic acid dissolved in 40ml of the aforementioned mixed solvent. Colorless crystals were precipitated during the dropwise addition, and the reaction was continued for 2.5 hours after the addition was completed. Suction filtration, wash the filter cake with 20ml of mixed solvent, and vacuum-dry at below 50°C for 6 hours to obtain 13.2g of amlodipine besylate with a yield of 95.2%. All indicators of the product meet the existing drug standards.

Embodiment 2

[0019] Mix 99% isopropyl acetate and 99% isopropanol according to the volume ratio of 1:1 to form a mixed solvent.

[0020] Dissolve 10g of amlodipine base (24.46mmol) in 80ml of the aforementioned mixed solvent, maintain the temperature at 0-5°C, and slowly add dropwise 4g (25.3mmol) of anhydrous benzenesulfonic acid dissolved in 40ml of the aforementioned mixed solvent. Colorless crystals were precipitated during the dropwise addition, and the reaction was continued for 2.5 hours after the addition was completed. Suction filtration, wash the filter cake with 20ml of mixed solvent, and vacuum-dry at below 50°C for 6 hours to obtain 12.5g of amlodipine besylate with a yield of 90.1%.

Embodiment 3

[0022] Mix 99% isopropyl acetate and absolute ethanol in a volume ratio of 1:1 to form a mixed solvent.

[0023] Dissolve 10g of amlodipine base (24.46mmol) in 80ml of the aforementioned mixed solvent, maintain the temperature at 0-5°C, and slowly add dropwise 4g (25.3mmol) of anhydrous benzenesulfonic acid dissolved in 40ml of the aforementioned mixed solvent. Colorless crystals were precipitated during the dropwise addition, and the reaction was continued for 2.5 hours after the addition was completed. Suction filtration, wash the filter cake with 20 ml of mixed solvent, and vacuum-dry at below 50° C. for 6 hours to obtain amlodipine besylate 12.0, with a yield of 86.5%.

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Abstract

This invention relates to medicine chemical field, concretely relates to benzene monsulfonic acid ammonia chlorine horizon preparation method. The ammonia chlorine horizon is reacted with benzene monsulfonic acid in component organic solvent of ester and alcohol. Its preparation method and operation technique is simple, yield is high, and product quality is easy to control.

Description

technical field [0001] The invention relates to the field of medicinal chemistry, in particular to a preparation method of amlodipine besylate. Background technique [0002] Amlodipine (amlodipine, structural formula I) has been widely used clinically as an effective calcium channel antagonist. It exhibits significant selectivity to arteriolar resistance and coronary artery resistance, and is mainly used clinically for the treatment of arterial hypertension. In further research on amlodipine, it is found that the addition salt of amlodipine and besylate and amlodipine besylate (structural formula II) have excellent solubility, stability, non-hygroscopicity and are beneficial to the preparation Advantages of the preparation. [0003] [0004] The method for preparing amlodipine besylate reported in the prior art mainly contains two kinds: [0005] Method 1: In CN87102493A, amlodipine and benzenesulfonic acid are reacted in methyl alcohol, and the yield is 83.3%. [000...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D211/90A61K31/4422A61P9/12
Inventor 于鑫
Owner SUZHOU DAWNRAYS PHARM CO LTD
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