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10.1021/acs.orglett.0c03052

http://scihub22266oqcxt.onion/10.1021/acs.orglett.0c03052
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33085486!7653677!33085486
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suck abstract from ncbi


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pmid33085486      Org+Lett 2020 ; 22 (21): 8430-8435
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  • Cyanoamidine Cyclization Approach to Remdesivir s Nucleobase #MMPMID33085486
  • Knapp RR; Tona V; Okada T; Sarpong R; Garg NK
  • Org Lett 2020[Nov]; 22 (21): 8430-8435 PMID33085486show ga
  • We report an alternative approach to the unnatural nucleobase fragment seen in remdesivir (Veklury). Remdesivir displays broad-spectrum antiviral activity and is currently being evaluated in Phase III clinical trials to treat patients with COVID-19. Our route relies on the formation of a cyanoamidine intermediate, which undergoes Lewis acid-mediated cyclization to yield the desired nucleobase. The approach is strategically distinct from prior routes and could further enable the synthesis of remdesivir and other small-molecule therapeutics.
  • |Adenosine Monophosphate/*analogs & derivatives/chemical synthesis/chemistry/therapeutic use[MESH]
  • |Alanine/*analogs & derivatives/chemical synthesis/chemistry/therapeutic use[MESH]
  • |Amidines/*chemistry[MESH]
  • |Antiviral Agents/*chemical synthesis/*chemistry/therapeutic use[MESH]
  • |COVID-19[MESH]
  • |Chemistry Techniques, Synthetic[MESH]
  • |Coronavirus Infections/drug therapy[MESH]
  • |Cyclization[MESH]
  • |Pandemics[MESH]


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