- Synthesis and antiviral evaluation of the 2'-c-methyl branched derivative of a nucleoside analog inhibitor of RNA viral infections, T-1106
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An example of a 2'-C-methyl branched nucleoside analogue bearing 3,4-dihydro-3-oxopyrazine-2-carboxamide as the base, namely 4-(2-C-methyl- β-D-ribofuranosyl)-3-oxo-3,4-dihydropyrazine-2-carboxamide, is reported. This compound was synthesized following a Vorbrueggen's glycosylation procedure in a few steps. When evaluated in cell culture experiments against a broad range of viruses, this compound did not exhibit any significant antiviral effect or cytotoxicity.
- Pierra, Claire,Counor, Clement,Storer, Richard,Gosselin, Gilles
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- METHODS FOR PREPARING FAVIPIRAVIR
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The present invention provides methods for preparing Favipiravir (6-fluoro-3-hydroxypyrazine-2-carboxamide).
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Paragraph 0023; 0335
(2021/11/20)
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- Synthesis process of favipiravir and intermediate thereof
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The invention relates to the technical field of medicine synthesis, and in particular, relates to a synthesis process of favipiravir and an intermediate thereof. The synthesis method of favipiravir comprises the following steps: 1) 2-aminopropanediamide and glyoxal serve as raw materials, and generating a compound III through a cyclization reaction; 2) performing benzyl protection on the compoundIII under the catalysis of potassium carbonate to generate a compound IV; 3) performing fluorine substitution on the compound IV under the action of fluorine gas, a solvent and a catalyst to generatea compound V; and 4) performing debenzylation protection on the compound V to generate favipiravir. Compared with other synthetic routes of favipiravir, the synthetic route provided by the invention has the advantages that the whole process route is shortened by virtue of high-selectivity fluorination reaction, the production cost is greatly reduced, and the synthesis process is suitable for industrial production.
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Paragraph 0044-0048
(2020/07/15)
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- 6-BROMO-3-HYDROXY-2-PYRAZINECARBOXAMIDE CRYSTAL AND METHOD FOR PRODUCING SAME
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The purpose of the present invention is to provide a method for producing 6-bromo-3-hydroxy-2-pyrazinecarboxamide in which the content ratio of impurities is reduced. This production method includes a step of obtaining 6-bromo-3-hydroxy-2-pyrazinecarboxamide crystal having diffraction angles expressed in degrees 20 of 5.5, 20.1, 23.7, 26.7, 27.5, and 28.1° and/or diffraction angles expressed in degrees 2θ of 7.1, 21.4, 25.2, 25.7, 27.1, and 28.8° in powder X-ray diffraction.
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Paragraph 0215; 0216; 0217; 0218; 0219; 0220; 0221; 0222
(2018/06/04)
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- 3-hydroxy-2-production of pyrazinecarboxamide
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PROBLEM TO BE SOLVED: To provide an excellent method for producing 3-hydroxy-2-pyrazinecarboxamide. SOLUTION: This method has characteristics that (1) the reaction temperature is normal temperature, (2) the yield is high, (3) the operation is simple, and the like, and is useful as an industrial production method of 3-hydroxy-2-pyrazinecarboxamide or a salt thereof. COPYRIGHT: (C)2011,JPOandINPIT
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Paragraph 0024
(2017/01/31)
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- NUCLEOSIDES WITH NON-NATURAL BASES AS ANTI-VIRAL AGENTS
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A method and composition for treating a host infected with flavivirus, pestivirus or hepacivirus comprising administering an effective fiavivirus, pestivirus or hepacivirus treatment amount of a described base- modified nucleoside or a pharmaceutically acceptable salt or prodrug thereof, is provided.
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Page/Page column 129-130
(2008/06/13)
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