Expedient Synthesis of Antiviral Drug Molnupiravir from D-Ribose and Cytosine

30 January 2024, Version 1
This content is a preprint and has not undergone peer review at the time of posting.

Abstract

Molnupiravir, an approved antiviral drug for treating SARS-CoV-2-infected patients, presents a critical need for a concise and sustainable synthesis from readily available raw materials due to its potential high demand. Herein, we report a cost-effective scalable synthetic route for the API by exploiting mild N-glycosylation conditions utilizing metal-free activation of an alkynyl carbonate donor. The overall yield is increased up to 48% using minimum purification and sequential one-pot reaction.

Keywords

Molnupiravir
Glycosylation
Nucleobase
N-glycosylation
Au-Ag catalysis

Supplementary materials

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Description
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Supplementary Data
Description
General procedures, Characterization Data, Mass and NMR spectra are reported
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