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[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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?:doi
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?:doi
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10.1021/acs.orglett.0c03052
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document_parses/pdf_json/edb9695214723cc57fb55cf4adfabdb178783255.json; document_parses/pdf_json/b00f29547e698e5d0e1f7d2d115525c194851ec0.json
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document_parses/pmc_json/PMC7653677.xml.json
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?:title
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Cyanoamidine Cyclization Approach to Remdesivir’s Nucleobase
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