Selected article for: "alternative approach and small molecule"

Author: Knapp, Rachel R.; Tona, Veronica; Okada, Taku; Sarpong, Richmond; Garg, Neil K.
Title: Cyanoamidine Cyclization Approach to Remdesivir’s Nucleobase
  • Cord-id: 3i2y230x
  • Document date: 2020_10_21
  • ID: 3i2y230x
    Snippet: [Image: see text] 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
    Document: [Image: see text] 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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