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
Title | Year | Author | Number |
---|---|---|---|
METHOD FOR SYNTHESISING DISODIUM SALT OF DEXAMETHASONE 21-PHOSPHATE APPLIED FOR TREATING PATIENTS WITH CORONAVIRUS INFECTION (COVID-19) | 2020 |
|
RU2764597C1 |
METHOD FOR OBTAINING 6α, 9α-DIFLUOR- 17α-(1-OXO-PROPOXY)-11β-HYDROXY-16α-METHYL-3-OXO-ANDROST-1,4-DIENE-17β-CARBOTHIONE ACID | 2003 |
|
RU2333217C2 |
METHOD OF OBTAINING 11BETA, 17 ALPHA, 21-TRIHYDROXY-16ALPHA-METHYL-9ALPHA-FLUOROPREGNA-1,4-DIENE-3,20-DIONE (DEXAMETHAZONE) FROM PHYTOSTEROL | 2013 |
|
RU2532902C1 |
METHOD FOR OBTAINING FLUTICASONE PROPIONATE OBTAINING, PARTICULARLY POLYMORPHOUS FORM 1 | 2003 |
|
RU2333218C2 |
16α,17a-ACETAL-SUBSTITUTED ANDROSTANE-17b-CARBOXYLIC ACID ESTERS OR THEIR STEREOISOMERS | 1991 |
|
RU2081879C1 |
DERIVATIVES OF ANDROSTENE, PHARMACEUTICAL COMPOSITION | 1997 |
|
RU2194053C2 |
METHOD OF PRODUCING 3β-ACETOXY-17α-HYDROPEROXY-16α-METHYLPREGNANES FROM Δ-20-KETOSTEROIDS AND METHOD OF PRODUCING 3β-ACETOXY-17α-HYDROXY-16α-METHYLPREGNANES USING 3β-ACETOXY-17α-HYDROPEROXY-16α-METHYLPREGNANES | 2009 |
|
RU2418805C1 |
SPECIFIC GLYCOCOTRICOSTEROID COMPOUND WITH ANTIINFLAMMATORY EFFECT | 2004 |
|
RU2348645C2 |
CHEMICAL COMPOUNDS | 2008 |
|
RU2462472C2 |
PREGNANE DERIVATIVES SUBSTITUTED IN 17-POSITION, METHOD OF THEIR SYNTHESIS, INDUSTRIAL PRODUCTS, PHARMACEUTICAL COMPOSITION | 1997 |
|
RU2177951C2 |
Authors
Dates
2022-03-29—Published
2021-06-29—Filed