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Cyanoamidine Cyclization Approach to Remdesivir's Nucleobase.
Knapp, Rachel R; Tona, Veronica; Okada, Taku; Sarpong, Richmond; Garg, Neil K.
Afiliação
  • Knapp RR; Department of Chemistry and Biochemistry, University of California, Los Angeles, California 90095-1569, United States.
  • Tona V; Department of Chemistry and Biochemistry, University of California, Los Angeles, California 90095-1569, United States.
  • Okada T; Department of Chemistry, University of California, Berkeley, California 94720, United States.
  • Sarpong R; Department of Chemistry, University of California, Berkeley, California 94720, United States.
  • Garg NK; Department of Chemistry and Biochemistry, University of California, Los Angeles, California 90095-1569, United States.
Org Lett ; 22(21): 8430-8435, 2020 11 06.
Article em En | MEDLINE | ID: mdl-33085486
ABSTRACT
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.
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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Antivirais / Monofosfato de Adenosina / Alanina / Amidinas Idioma: En Ano de publicação: 2020 Tipo de documento: Article
Texto completo
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PubMed Links
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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Antivirais / Monofosfato de Adenosina / Alanina / Amidinas Idioma: En Ano de publicação: 2020 Tipo de documento: Article