FIELD: chemistry.
SUBSTANCE: invention relates to a novel improved method of producing entecavir of formula (I) which has antiviral effect for possible use in a medicinal agent with low content of the active component, for example in treating hepatitis B. The invention also relates to novel intermediate products and their methods of production. The entecavir has general formula (I) . Its method of production involves subjecting a compound of formula 7c or its mixture with a compound of formula 8a, where Rb is C1-C4alkyl, to oxidation, mainly with a peroxidate, such as a sodium carbonate peroxidate, sodium pyrophosphate peroxidate etc. 7c + 8a. Compound of formula 7c or its mixture with a compound of formula 8a is obtained by bringing the compound of formula 7a into contact with at least one acid selected from halogenated methane-sulphonic acid and possibly methane-sulphonic acid, possibly in the presence of a compound of formula 8a, with subsequent treatment with at least one aqueous base. The invention also relates to production of compounds of formulae 7a and 8a.
EFFECT: increased antiviral effect of the compounds.
27 cl, 8 dwg, 19 ex
Title | Year | Author | Number |
---|---|---|---|
{3-[(7H-PYRROLO[2,3-d]PYRIMIDIN-4-YL)AZOLYL]AZETIDIN-3-YL} ACETONITRILES AS JANUS KINASE INHIBITORS | 2015 |
|
RU2601410C1 |
METHOD OF MYOCARDIAL BLOOD PERFUSION IMAGING | 2012 |
|
RU2648358C2 |
FIBROBLAST ACTIVATION PROTEIN INHIBITORS | 2020 |
|
RU2802426C2 |
BENZOFUSED COMPOUNDS, PHARMACEUTICAL COMPOSITION BASED ON THEREOF, METHOD OF THEIR SYNTHESIS AND A METHOD OF SYNTHESIS OF AN INTERMEDIATE COMPOUND | 1992 |
|
RU2114110C1 |
SUBSTITUTED 2-METHYLIDEN-5-(PHENYLAMINO)-2,3-DIHYDROTIOPHEN-3-ONE FOR TREATMENT OF LEUKEMIAS WITH TRANSLOCATIONS OF MLL-GENE AND OTHER ONCOLOGICAL DISEASES | 2017 |
|
RU2656603C1 |
CXCR7 ANTAGONISTS | 2013 |
|
RU2649004C2 |
SPIRO COMPOUNDS AS ERK INHIBITORS AND THEIR USE | 2020 |
|
RU2800042C1 |
NOVEL PEPTIDE DERIVATIVES AND USE THEREOF | 2015 |
|
RU2699572C2 |
SUBSTITUTED 3,4,12,12A-TETRAHYDRO-1H-[1,4]OXAZINO[3,4-C]PYRIDO[2,1-F][1,2,4]TRIAZINE-6,8-DIONE, PHARMACEUTICAL COMPOSITION, METHODS FOR PRODUCTION AND USE THEREOF | 2019 |
|
RU2720305C1 |
1,3,4-OXADIAZOLE DERIVATIVES AS HISTONE DEACETYLASE 6 INHIBITOR AND PHARMACEUTICAL COMPOSITION CONTAINING THEM | 2019 |
|
RU2763936C1 |
Authors
Dates
2010-03-20—Published
2005-06-03—Filed