A High-Yielding Synthesis of EIDD-2801 from Uridine

07 October 2020, Version 1
This content is a preprint and has not undergone peer review at the time of posting.

Abstract

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.

Keywords

EIDD-2801
COVID-19
continuous flow
acetonide deprotection
triazolation

Supplementary materials

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Title
EIDD-2801 SI ChemRxiv
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