ArticleACS omega2021
Progress Toward a Large-Scale Synthesis of Molnupiravir (MK-4482, EIDD-2801) from Cytidine.
Article in ACS omega, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 18 papers.
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Who cites it
18 citing papers in PubMed.
- 1'-Cyanocytidine-5'-isobutyryl is a potent SARS-CoV-2 inhibitor in culture and infected Syrian hamsters.Science advances · 2025Article
- Scaling the Process Chemistry of a COVID-19 Antiviral Pharmaceutical Down for a Multistep Synthesis Experiment in the Undergraduate Teaching Laboratory.Journal of chemical education · 2024Article
- Article
- Molnupiravir: A Versatile Prodrug against SARS-CoV-2 Variants.Metabolites · 2023Review
- Article
- Development and validation of molnupiravir assessment in bulk powder and pharmaceutical formulation by the RP-HPLC-UV method.RSC advances · 2022Article
- Pharmacological treatment of COVID-19: an opinion paper.Revista espanola de quimioterapia : publicacion oficial de la Sociedad Espanola de Quimioterapia · 2022Review
- An Engineered Cytidine Deaminase for Biocatalytic Production of a Key Intermediate of the Covid-19 Antiviral Molnupiravir.Journal of the American Chemical Society · 2022Article
- Current Insights and Molecular Docking Studies of the Drugs under Clinical Trial as RdRp Inhibitors in COVID-19 Treatment.Current pharmaceutical design · 2022Article
- Minimum Manufacturing Costs, National Prices, and Estimated Global Availability of New Repurposed Therapies for Coronavirus Disease 2019.Open forum infectious diseases · 2022Article
- Review on molnupiravir as a promising oral drug for the treatment of COVID-19.Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents · 2022Review
- Cost of Goods Analysis Facilitates an Integrated Approach to Identifying Alternative Synthesis Methodologies for Lower Cost Manufacturing of the COVID-19 Antiviral Molnupiravir.Gates open research · 2022Article
- Molnupiravir and Its Antiviral Activity Against COVID-19.Frontiers in immunology · 2022Review
- Engineered Ribosyl-1-Kinase Enables Concise Synthesis of Molnupiravir, an Antiviral for COVID-19.ACS central science · 2021Article
- Toward a Practical, Nonenzymatic Process for Investigational COVID-19 Antiviral Molnupiravir from Cytidine: Supply-Centered Synthesis.Organic process research & development · 2021Review
- Conversion ofRSC advances · 2021Article
- Short Synthesis of Molnupiravir (EIDD-2801)ACS omega · 2021Article
- Comparative molecular docking and simulation analysis of molnupiravir and remdesivir with SARS-CoV-2 RNA dependent RNA polymerase (RdRp).Bioinformation · 2021Article
Corrections and comments
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Authors and funding
9 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Molnupiravir (MK-4482, EIDD-2801) is a promising orally bioavailable drug candidate for the treatment of COVID-19. Herein, we describe a supply-centered and chromatography-free synthesis of molnupiravir from cytidine, consisting of two steps: a selective enzymatic acylation followed by transamination to yield the final drug product. Both steps have been successfully performed on a decagram scale: the first step at 200 g and the second step at 80 g. Overall, molnupiravir has been obtained in a 41% overall isolated yield compared to a maximum 17% isolated yield in the patented route. This route provides many advantages to the initial route described in the patent literature and would decrease the cost of this pharmaceutical should it prove safe and efficacious in ongoing clinical trials.
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Registered trials
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