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Synthesis and antiviral evaluation of 1′-cyano-3′-deoxy-3′-fluoro pyrimidine nucleos(t)ide analogs
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DOI：10.1016/j.tetlet.2026.156006.png)
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Abstract
En 中文
Nucleoside and nucleotide analogs remain the cornerstone of antiviral therapy. Herein, we report the synthesis of novel 1 '-cyano-3 '-fluoro-substituted pyrimidine nucleoside analogs and their corresponding phosphoramidate prodrugs. A 1-bromo-1-cyano-3-fluoro ribosyl donor was coupled with different silylated nucleobases using a silver triflate mediated Vorbr & uuml;ggen reaction. Following deprotection, the resulting 1 '-cyano-3 '-fluoro-substituted nucleosides 12a-d were reacted with the chiral pentafluorophenyl reagent to afford the corresponding phosphoramidate prodrugs 14a-d. All synthesized compounds were evaluated against a panel of DNA and RNA viruses, including human cytomegalovirus (HCMV), varicella-zoster virus (VZV), severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), human coronavirus 229E (HCoV-229E) and influenza viruses.
Keywords:
Nucleoside
Nucleotide
Prodrug
Antiviral
Drug discovery
Journal
T
IF:
1.5
Papers:
148
Citations:
4.2W
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Cited Papers