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A High‐Yielding Synthesis of EIDD‐2801 from Uridine **
Author(s) -
Steiner Alexander,
Znidar Desiree,
Ötvös Sándor B.,
Snead David R.,
Dallinger Doris,
Kappe C. Oliver
Publication year - 2020
Publication title -
european journal of organic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.825
H-Index - 155
eISSN - 1099-0690
pISSN - 1434-193X
DOI - 10.1002/ejoc.202001340
Subject(s) - chemistry , uridine , yield (engineering) , selectivity , combinatorial chemistry , acetonide , sequence (biology) , chromatography , organic chemistry , rna , biochemistry , surgery , medicine , materials science , triamcinolone acetonide , metallurgy , gene , catalysis
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.