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A High‐Yielding Synthesis of EIDD‐2801 from Uridine**

Alexander Steiner, Desiree Znidar, Sándor B. Ötvös, David R. Snead, Doris Dallinger, C. Oliver Kappe

2020European Journal of Organic Chemistry39 citationsDOIOpen Access PDF

Abstract

A simple reordering of the reaction sequence allowed the improved synthesis of EIDD-2801, an antiviral drug 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.

Topics & Concepts

ChemistryUridineYield (engineering)SelectivityCombinatorial chemistryAcetonideSequence (biology)ChromatographyOrganic chemistryRNABiochemistrySurgeryMetallurgyCatalysisMedicineMaterials scienceTriamcinolone acetonideGeneInnovative Microfluidic and Catalytic Techniques InnovationChemical Synthesis and AnalysisAnalytical Chemistry and Chromatography
A High‐Yielding Synthesis of EIDD‐2801 from Uridine** | Litcius