FIELD: organic chemistry; pharmaceuticals.
SUBSTANCE: group of inventions relates to a new method of producing sugammadex pharmaceutical product. The following is disclosed: a method of producing sugammadex including: dissolving 6-per-deoxy-6-bromo-γ-cyclodextrin in solvent; adding 3-mercaptopropionic acid to obtain a first solution; adding an aqueous base solution to the first solution at a rate sufficient to maintain the temperature of the resulting solution within a range of approximately 5 to 40°C; stirring the resulting solution while heating; adjusting the pH of the resulting mixture to 7–13 and isolating sugammadex as a product, where the solvent is 1-methyl-2-pyrrolidinone, and the base in an aqueous solution of the base is sodium hydroxide, sodium carbonate, sodium phosphate, sodium bis(trimethylsilyl)amide, tert-sodium butoxide or sodium tert-pentylate or a mixture thereof. In addition, a method of preparing sugammadex using a solubility-increasing reagent selected from the group consisting of sodium 4-tosylate, sodium 3-tosylate and sodium 2-tosylate in a mixture of THF and water is disclosed, and methods of preparing the starting 6-per-deoxy-6-bromo-γ-cyclodextrin.
EFFECT: group of inventions ensures the production of sugammadex in high yield.
31 cl, 4 ex
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Authors
Dates
2023-12-21—Published
2019-06-03—Filed