期刊
ORGANIC LETTERS
卷 22, 期 21, 页码 8430-8435出版社
AMER CHEMICAL SOC
DOI: 10.1021/acs.orglett.0c03052
关键词
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资金
- Bill and Melinda Gates Foundation [INV-005860]
- Max Kade Foundation
- Austrian Academy of Sciences (OAW)
- Astellas Foundation for Research on Metabolic Disorders
- NSF [CHE-1048804]
- NIH NCRR [S10RR025631]
- Trueblood Family
- Bill and Melinda Gates Foundation [INV-005860] Funding Source: Bill and Melinda Gates Foundation
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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