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A High-Yielding Synthesis of EIDD-2801 from Uridine

preprint
submitted on 07.10.2020 and posted on 07.10.2020 by Alexander Steiner, Desiree Znidar, Sándor B. Ötvös, David R. Snead, Doris Dallinger, C. Oliver Kappe
A simple reordering of the reaction sequence allowed the improved synthesis of EIDD-2801, an antiviral with promising activity against the SARS-CoV-2 virus, starting from uridine. Compared to the original route, the yield was enhanced from 17% to 61%, and fewer isolation/purification steps were needed. In addition, a continuous flow procedure for the final acetonide deprotection was developed, which proved to be favorable toward selectivity and reproducibility.

Funding

Bill and Melinda Gates Foundation

History

Email Address of Submitting Author

do.dallinger@uni-graz.at

Institution

University of Graz

Country

Austria

ORCID For Submitting Author

0000-0003-1649-0465

Declaration of Conflict of Interest

no conflict of interest

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