Ontology highlight
ABSTRACT:
SUBMITTER: Knapp RR
PROVIDER: S-EPMC7653677 | biostudies-literature | 2020 Nov
REPOSITORIES: biostudies-literature
Knapp Rachel R RR Tona Veronica V Okada Taku T Sarpong Richmond R Garg Neil K NK
Organic letters 20201021 21
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 remd ...[more]