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A High-Yielding Synthesis of EIDD-2801 from Uridine.

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.

SUBMITTER: Steiner A

PROVIDER: S-EPMC7894511 | biostudies-literature | 2020 Nov

REPOSITORIES: biostudies-literature

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A High-Yielding Synthesis of EIDD-2801 from Uridine.

Steiner Alexander A Znidar Desiree D Ötvös Sándor B SB Snead David R DR Dallinger Doris D Kappe C Oliver CO

European journal of organic chemistry 20201112 43

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. ...[more]

PMID: 33664631

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