Cyanoamidine Cyclization Approach to Remdesivir’s Nucleobase | Zendy

Rachel R. Knapp | Zendy; Veronica Tona | Zendy; Taku Okada | Zendy; Richmond Sarpong | Zendy; Neil K. Garg | Zendy

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Cyanoamidine Cyclization Approach to Remdesivir’s Nucleobase

Author(s) -

Rachel R. Knapp,

Veronica Tona,

Taku Okada,

Richmond Sarpong,

Neil K. Garg

Publication year - 2020

Publication title -

organic letters

Language(s) - Uncategorized

Resource type - Journals

SCImago Journal Rank - 1.94

H-Index - 239

eISSN - 1523-7060

pISSN - 1523-7052

DOI - 10.1021/acs.orglett.0c03052

Subject(s) - nucleobase , chemistry , yield (engineering) , combinatorial chemistry , covid-19 , molecule , stereochemistry , dna , virology , biochemistry , organic chemistry , biology , medicine , outbreak , materials science , disease , pathology , infectious disease (medical specialty) , metallurgy

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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