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Synthesis method of sodium sugammadex

A technology of sugammadex sodium and a synthetic method, which is applied in the field of preparation of muscle relaxant antagonist drugs, can solve the problems of inability to realize industrialization, large pollution, and low yield, and achieve easy industrial production, high yield, and good fat solubility Effect

Active Publication Date: 2018-02-13
河北坤安药业有限公司
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  • Abstract
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  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0012] The purpose of the present invention is to provide a synthetic method of sugammadex sodium to solve the problems of low yield, low purity, large pollution and inability to realize industrialization in the existing sugammadex sodium preparation method

Method used

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  • Synthesis method of sodium sugammadex
  • Synthesis method of sodium sugammadex
  • Synthesis method of sodium sugammadex

Examples

Experimental program
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Effect test

Embodiment 1

[0045] Synthesis of Compound III:

[0046] Add 100.00g of γ-cyclodextrin (dried at 105°C for 24h) and 1600mL of N,N-dimethylformamide into the reaction flask, stir to dissolve and raise the temperature to 65-75°C, drop 150.12g of methylsulfonate into the feed solution Acyl chloride, dropwise, keep stirring and react for 16-18h, then lower the temperature to 0°C, add sodium methoxide-methanol solution to the system to adjust the pH>10, pour the reaction solution into 3200mL water and stir for 30min, centrifuge, wash the filter cake with water, and dry to obtain 103.5 g of white solid compound III. Yield 99%, LC / MS ES - -Mass-to-core ratio of API [M-H] - = 1443.40.

[0047] Synthesis of Compound IV:

[0048]Add 300mL of pyridine and 200mL of acetic anhydride to 100.00g of compound III, stir and heat up to 60°C, keep warm at 55-65°C and stir for 6-8h, monitor by TLC, and cool down to room temperature after the raw material point disappears. Add 1200mL water to the system, st...

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Abstract

The invention provides a synthesis method of sodium sugammadex. The synthesis method includes: using gamma-cyclodextrin as a raw material, and subjecting the raw material sequentially to halogenationreaction, acetylation reaction, etherification reaction, alcoholysis and hydrolysis to obtain high-purity sodium sugammadex. Yield of the method is up to 70%, the method is simple in technical process, low in energy consumption, pollution-free, easy-to-get in raw materials, simple in industrial operation, low in cost, safe, environment-friendly and easy for industrial production, and sodium sugammadex up to higher than 99% in purity can be obtained without membrane dialysis operation.

Description

technical field [0001] The invention relates to a preparation method of muscle relaxant antagonist medicine, in particular to a synthesis method of sugammadex sodium. Background technique [0002] Sugammadex sodium (sugammadex sodium), the chemical name is eight-6-perdeoxy-6-perfect (2-carboxyethyl) thio-γ-cyclodextrin sodium salt, American Chemical Abstracts Registry Number CAS: 343306- 71-8, the structural formula is: [0003] [0004] Sugammadex sodium is a selective relaxation agent used to reverse the effect of muscle relaxants rocuronium bromide or vecuronium bromide, which was first discovered by Organon Biosciences in the Netherlands. On July 25, 2008, the European Medicines Agency has approved sugammadex sodium for marketing in Europe. On October 20, 2010, sugammadex sodium was approved for marketing in Japan. In November 2015, the FDA approved the drug for marketing in the United States. . At present, CFDA has approved the marketing of sugammadex sodium in Ch...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08B37/16
Inventor 李萍
Owner 河北坤安药业有限公司
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