- Scalable synthesis of favipiravir: Via conventional and continuous flow chemistry
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Decagram scale synthesis of favipiravir was performed in 9 steps using diethyl malonate as cheap starting material. Hydrogenation and bromination steps were achieved by employing a continuous flow reactor. The synthetic process provided a total of 16% yield and it is suitable for larger-scale synthesis and production. This journal is
- Charoensetakul, Netnapa,Khamkhenshorngphanuch, Thitiphong,Srikun, Onsiri,Srimongkolpithak, Nitipol,Thongpanchang, Chawanee,Tiyasakulchai, Thanat,Yuthavong, Yongyuth
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p. 38691 - 38693
(2021/12/20)
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- PERK INHIBITING IMIDAZOLOPYRAZINE COMPOUNDS
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Provided herein are compounds of formula (I) as shown below, compositions, and methods useful for inhibiting PERK and for treating related conditions, diseases, and disorders.
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Paragraph 0182; 0183
(2021/03/05)
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- PERK INHIBITING IMIDAZOLOPYRAZINE COMPOUNDS
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Provided herein are methods for treating a viral infection in a patient, comprising administering to said patient a therapeutically effective amount of a PERK inhibitor selected from a compound having the structure (I).
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Page/Page column 100
(2021/11/20)
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- PERK INHIBITING INDOLINYL COMPOUNDS
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Provided herein are compounds of formula (I), compositions, and methods useful for inhibiting PERK and for treating related conditions diseases, and disorders, wherein Q is selected from (Ia), (Ib) ou (Ic).
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Paragraph 0171; 0172
(2021/03/05)
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- Synthetic method of 2-aminomalononitrile
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The invention discloses a synthetic method of 2-aminomalononitrile. The synthetic method comprises the following steps of: 1) adopting aminomalonic acid diethyl ester as a starting material, directlyplacing into 40-60w/v% of ammonium-chloride aqueous solution, reacting for 2-5 hours at a temperature of 100-120 DEG C and preparing to obtain 2-aminopropanediamide; 2) dissolving 2-aminopropanediamide prepared in the step 1) into an organic solvent, heating to rise the temperature, adding solid phosgene, heating and refluxing for 10-12 hours to generate 2-aminomalononitrile. The synthetic methoddisclosed by the invention is simple, pollution-free, safe and environmentally friendly and provides basis for further application of 2-aminomalononitrile.
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Paragraph 0016; 0017; 0018; 0019
(2018/07/30)
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- BICYCLIC COMPOUNDS AS ALLOSTERIC SHP2 INHIBITORS
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The present disclosure is directed to inhibitors of SHP2 and their use in the treatment of disease. Also disclosed are pharmaceutical compositions comprising the same.
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Paragraph 00680
(2018/08/20)
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- 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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experimental part
p. 1327 - 1333
(2012/04/17)
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- SULFONIC ACID SALT COMPOUND OF 4-CARBAMOYL-5-HYDROXY-IMIDAZOLE DERIVATIVE
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The object is to provide a stable SM-108 derivative, which is effective as a carcinostatic agent, particularly an SM-108 derivative having good storage stability. An SM-108 compound having good storage stability can be produced by producing an organic sulfonic acid salt compound of SM-108. Further, a crystalline SM-108 compound containing a trace amount of an organic carboxylic acid can be produced by using an aqueous solution of the organic sulfonic acid salt of SM-108, and by adding an alkali metal salt of an organic carboxylic acid to the aqueous solution to neutralize the aqueous solution and then causing the crystal precipitation in the solution.
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Page/Page column 5; 6
(2010/07/03)
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- IMIDAZOPYRAZINE COMPOUNDS
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Novel imidazopyrazine compounds are disclosed that have a formula represented by the following: Formula (I). The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a viral infection, in particular a HCV, HRV, Sb and/or CVB in a patient in need thereof.
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Page/Page column 69
(2009/04/25)
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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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- SUBSTITUTED 4-AMINO-PYRROLOTRIAZINE DERIVATIVES USEFUL FOR TREATING HYPER-PROLIFERATIVE DISORDERS AND DISEASES ASSOCIATED WITH ANGIOGENESIS
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This invention relates to novel pyrrozolotriazine compounds, pharmaceutical compositions containing such compounds and the use of those compounds and compositions for the prevention and/or treatment of hyper-proliferative disorders and diseases associated with angiogenesis.
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Page/Page column 185
(2008/06/13)
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