METHOD FOR OBTAINING THE DISODIUM SALT OF DEXAMETHASONE 21-PHOSPHATE USED FOR THE TREATMENT OF PATIENTS WITH CORONAVIRUS INFECTION (COVID-19) Russian patent published in 2022 - IPC C07J5/00 A61K31/66 C07J75/00 C07F9/09 

Abstract RU 2769195 C1

FIELD: pharmaceutics.

SUBSTANCE: invention relates to a method for producing the disodium salt of dexamethasone 21-phosphate (11β,17α-dihydroxy-9α-fluoro-16α-methyl-21-(phosphonooxy)pregna-1,4-diene-3,20-dione), according to formula I

from the 21-halide derivative of 21-deoxy-dexamethasone: 21-iodide or 21-bromide 11β,17α-dihydroxy-9α-fluoro-16α-methylpregna-1,4-diene-3,20-dione, involving the substitution reaction of a halogen atom for a phosphonooxy group using 85% orthophosphoric acid in the presence of an organic base, removal of steroid impurities from an aqueous reaction medium by liquid-phase extraction with chlorocarbon, extraction of dexamethasone 21-phosphate from the aqueous reaction medium by solid-phase extraction using nonionic macroporous polymers, desorption with a mixture of organic solvents containing chlorocarbon and aliphatic alcohol, reaction of 21-dexamethasone phosphate with sodium alcoholate in an aliphatic alcohol medium, and the disodium salt of dexamethasone 21-phosphate can be obtained without the release of dexamethasone 21-phosphate.

EFFECT: expansion of the range of solutions against coronavirus.

17 cl, 6 ex

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RU 2 769 195 C1

Authors

Savinova Tatyana Stepanovna

Kazantsev Aleksej Vitalevich

Lukashev Nikolaj Vadimovich

Dates

2022-03-29Published

2021-06-29Filed