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Method for preparing high-purity sugammadex

A technology of high-purity sugammadex sodium, applied in the field of medicine, can solve the problems of safety, difficulty in preparing high-quality sugammadex sodium, and achieves improved quality and yield, significant industrial application value, purification Efficient effect

Inactive Publication Date: 2017-05-31
CHENGDU SOURCEBIO LIMITED LIABILITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0012] In summary, due to the structural characteristics of sugammadex sodium itself, a large number of impurities with similar physical and chemical properties are produced during the synthesis process. These impurities are difficult to prepare high Quality Sugammadex Sodium
In addition, most of the currently published sugammadex sodium synthesis methods are based on the reaction of 6-perdeoxy-6-perhalogenated-γ-cyclodextrin and mercaptopropionic acid in the presence of a flammable and explosive alkaline reagent, sodium hydride. Done, there are serious security issues in industrial applications

Method used

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  • Method for preparing high-purity sugammadex

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Experimental program
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Embodiment 1

[0032]

[0033] Under the conditions of ice bath and nitrogen protection, sodium hydroxide (4.4 g, 0.11 mol) was dispersed in 100 mL of N,N-dimethylformamide, and 3-mercaptopropionic acid (5.3 g, 0.05 mol) was slowly added dropwise, Keep the temperature at 0-5°C. After the dropwise addition was completed, the temperature was raised to room temperature, and the reaction was continued for 30 minutes. Cool down to 0°C again, slowly add 6-perdeoxy-6-periodo-γ-cyclodextrin (10.9 g, 5 mmol) in N,N-dimethylformamide solution dropwise, and raise the temperature to 80°C after the addition Reaction 20h. Concentrate the reactant under reduced pressure to a small volume, add 20 mL of water and 150 mL of ethanol to disperse, stir, and filter to obtain 8.3 g of a crude product with a yield of 76%.

Embodiment 2

[0035]

[0036] Under the conditions of ice bath and nitrogen protection, sodium hydroxide (4.4 g, 110 mmol) was dispersed in 100 mL of N,N-dimethylformamide, and 3-mercaptopropionic acid (5.3 g, 50 mmol) was slowly added dropwise to keep the temperature at 0-5°C. After the dropwise addition was completed, the temperature was raised to room temperature, and the reaction was continued for 30 minutes. Cool down to 0°C again, slowly add 6-perdeoxy-6-perbromo-γ-cyclodextrin (9 g, 5 mmol) in N,N-dimethylformamide solution dropwise, and raise the temperature to 80°C after the addition Reaction 20h. Concentrate the reactant under reduced pressure to a small volume, add 20 mL of water, and 150 mL of ethanol to disperse, stir, and filter to obtain 7.7 g of crude product, with a yield of 71%.

Embodiment 3

[0038]

[0039]Under the conditions of ice bath and nitrogen protection, sodium hydroxide (4.4 g, 110 mmol) was dispersed in 100 mL of N,N-dimethylformamide, and 3-mercaptopropionic acid (5.3 g, 50 mmol) was slowly added dropwise to keep the temperature at 0-5°C. After the dropwise addition was completed, the temperature was raised to room temperature, and the reaction was continued for 30 minutes. Cool down to 0°C again, slowly add 6-perdeoxy-6-perbromo-γ-cyclodextrin (7.2 g, 5 mmol) in N,N-dimethylformamide solution dropwise, and raise the temperature to 100°C after the addition Anti-24 hours. Concentrate the reactant under reduced pressure to a small volume, add 20 mL of water and 150 mL of ethanol to disperse, stir, and filter to obtain 6.7 g of a crude product with a yield of 62%.

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Abstract

The invention discloses a method for preparing high-purity sugammadex. The product purity is greater than 98%, the method comprises the following steps: 1) 6-deoxy-6-perhalogeno-gamma-cyclodextrin, mercaptopropionic acid and an alkalescence reagent are reacted at a certain reaction temperature in a reaction solvent to obtain a crude product sugammadex; and 2) re-crystallizing the crude product in the above step and purifying to obtain the sugammadex with purity greater than more than 98%. The method has the advantages of short synthesis step, simple technology and high security , high product quality, and large scale production.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a preparation and purification method of sugammadex sodium, a muscle relaxant reversal agent. Background technique [0002] Sugammadex, trade name Bridion (Bridion), is a new type of muscle relaxant reversal agent developed by Organon Biotechnology Company in the Netherlands, and is a chemical modification of cyclodextrin. The drug was approved for marketing by the European Union in 2008. Its mechanism of action is: selectively wrapping the steroidal neuromuscular stagnation drugs rocuronium bromide and vecuronium bromide to form a 1:1 ratio of inactive tight water-soluble complexes, thereby Blocks the action of muscle relaxants without the side effects associated with anticholinesterase drugs. The results of clinical studies show that it can immediately reverse the effect of rocuronium bromide used by adults, and routinely reverse the effect of rocuronium bromide u...

Claims

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Application Information

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IPC IPC(8): C08B37/16
CPCC08B37/0012
Inventor 张琴
Owner CHENGDU SOURCEBIO LIMITED LIABILITY
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