Results: The target compound was efficiently prepared by the above synthetic route. incorporation of nucleotides. :128-130 °C (Lit. Primer extension analysis demonstrated In the first A series of novel 3-methyl-7-substituted-4H-1,4-benzothiazine-2-carbohydrazide (3a-e) and corresponding thiosemicarbazide (4a-q) have been synthesized from 2-amino-5-substituted-thiophenol (1a-e) through the synthesis of 2-carboethoxy-3-methyl-7-substituted-1,4-benzothiazine (2a-e). Compounds F 3 and F 4 showed remarkable antibacterial activities against Staphylococcus aureus and Escherichia coli bacteria. Shandong Qidu PharmaceuticalCo., Ltd., Linzi 255400; 2.
Clin Infect Dis 6310:1288–1294. Favipiravir was synthesized in only six steps from 3-aminopyrazine-2-carboxylic acid with an overall yield of about 22.3%. A Phase III clinical evaluation of favipiravir for influenza therapy has been completed in Japan and two Phase II studies have been completed in the United States. Beldar SV, Jordis U (2009) Synthetic studies towards the antiviral pyrazine derivative T-705. Currently, neither a vaccine nor an effective antiviral treatment is available for use in humans. sulfuryl chloride, phosphoryl chloride, phosphorus trichloride or phosphorus pentachloride. A facile route for the synthesis of Bai CQ, Mu JS, Kargbo D, Song YB, Niu WK, Nie WM, Kanu A, Liu WW, Wang YP, Dafae F, Yan T, Hu Y, Deng YQ, Lu HJ, Yang F, Zhang XG, Sun Y, Cao YX, Su HX, Sun Y, Liu WS, Wang CY, Qian J, Liu L, Wang H, Tong YG, Liu ZY, Chen YS, Wang HQ, Kargbo B, Gao GF, Jiang JF (2016) Clinical and virological characteristics of Ebola virus disease patients treated with favipiravir (T-705)-Sierra leone, 2014. Antivir Res 823:95–102. : 112–114 °C (Lit.
In the key synthetic reaction, 3,6-dichloropyrazine-2-carbonitrile (6) was reacted sequentially, in one pot, with KF and 30% H2O2 to give (after crystallization from 95% EtOH) favipiravir as colorless crystals, with a 60% yield for this final step of the synthesis.Outbreaks of Ebola hemorrhagic fever in sub-Saharan Africa are associated with case fatality rates of up to 90%. Enzyme kinetic analysis demonstrated that T-705RTP inhibited the incorporation of ATP and GTP in In addition to its anti-influenza activity, favipiravir blocks the replication of many other RNA viruses, including arenaviruses (Junin, Machupo and Pichinde); phleboviruses (Rift Valley fever, sandfly fever and Punta Toro); hantaviruses (Maporal, Dobrava, and Prospect Hill); flaviviruses (yellow fever and West Nile); enteroviruses (polio- and rhinoviruses); an alphavirus, Western equine encephalitis virus; a paramyxovirus, respiratory syncytial virus; and noroviruses. You can also search for this author in The structures of these compounds have been elucidated by spectral IR and 1 H-NMR analysis. Like the experimental antiviral drugs T-1105 and T-1106, it is a pyrazinecarboxamide derivative.. Yield: 55%, off-white solid, M.p. Authors: Qi Guo.
The new synthetic approach to favipiravir starting from 2-aminopyarzine Our synthetic approach to favipiravir in this paper and the preferred route was highlighted in redWith respect to the first step, at the beginning, mono-chlorination of Another synthetic approach to favipiravir proposed in this paperIn summary, we investigated the synthesis of favipiravir starting from an inexpensive and commercially available 2-aminopyrazine.
Gao J, Luo X, Li Y, Gao R, Chen H, Ji D (2018) Synthesis and biological evaluation of 2-oxo-pyrazine-3-carboxamide-yl nucleoside analogues and their epimers as inhibitors of influenza a viruses. virus in vitro and in vivo. these inhibitory mechanisms, we analyzed the enzyme kinetics of inhibition using Lineweaver-Burk plots of four natural nucleoside Compounds 3b,c can be cyclized in high yields to 4b,c in 5% sodium hydroxide solution. Some features of the site may not work correctly.Favipiravir was first synthesized from an inexpensive and commercially available starting material, 2-aminopyrazine. The complete synthesis of favipiravir from 2-aminopyrazine.
Conclusions Among patients with COVID-19, Favipiravir, compared … No difference was observed of AOT or NMV rate (both P>0.05). Favipiravir was first synthesized from an inexpensive and commercially available starting material, 2-aminopyrazine. January 2019; DOI: 10.1007/s11696-018-0654-9. Sangawa H, Komeno T, Nishikawa H, Yoshida A, Takahashi K, Nomura N, Furuta Y (2013) Mechanism of action of T-705 ribosyl triphosphate against influenza virus RNA polymerase. The first step, cyclization to a 2-substituted-4-chloromethyl-4-hydroxythiazoline is carried out in the presence of bicarbonate in an aprotic solvent.
This work was supported by National Science Foundation for Young Scientists of China (Grant no. The bioavailability of favipiravir is almost complete at 97.6%. To elucidate 113–114 °C, Sato et al. The product of aminolysis was cyclized with glyoxal to yield 3-hydroxy-2-pyraziamide, which was subjected to nitration with KNO3, chlorination and dehydration with POCl3 and fluorination with KF to afford 3, 6-difluoropyrazin-2-carbonnitrile. Favipiravir is active against a broad range of influenza viruses, including A(H1N1)pdm09, A(H5N1) and the recently emerged A(H7N9) avian virus.
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