Progress Towards a Large-Scale Synthesis of Molnupiravir (MK-4482, EIDD-2801) from Cytidine Article Swipe
YOU?
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· 2021
· Open Access
·
· DOI: https://doi.org/10.26434/chemrxiv.13809527
Molnupiravir (MK-4482, EIDD-2801) is a promising orally bioavailable drug candidate for 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 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.
Related Topics
- Type
- preprint
- Language
- en
- Landing Page
- https://doi.org/10.26434/chemrxiv.13809527
- https://chemrxiv.org/engage/api-gateway/chemrxiv/assets/orp/resource/item/60c754ff9abda2432ff8e284/original/progress-towards-a-large-scale-synthesis-of-molnupiravir-mk-4482-eidd-2801-from-cytidine.pdf
- OA Status
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- References
- 10
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- OpenAlex ID
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Raw OpenAlex JSON
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https://openalex.org/W4232818755Canonical identifier for this work in OpenAlex
- DOI
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https://doi.org/10.26434/chemrxiv.13809527Digital Object Identifier
- Title
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Progress Towards a Large-Scale Synthesis of Molnupiravir (MK-4482, EIDD-2801) from CytidineWork title
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preprintOpenAlex work type
- Language
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enPrimary language
- Publication year
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2021Year of publication
- Publication date
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2021-02-16Full publication date if available
- Authors
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Grace P. Ahlqvist, Catherine P. McGeough, Chris H. Senanayake, Joseph D. Armstrong, Ajay Yadaw, Sarabindu Roy, Saeed Ahmad, David Snead, Timothy F. JamisonList of authors in order
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https://doi.org/10.26434/chemrxiv.13809527Publisher landing page
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https://chemrxiv.org/engage/api-gateway/chemrxiv/assets/orp/resource/item/60c754ff9abda2432ff8e284/original/progress-towards-a-large-scale-synthesis-of-molnupiravir-mk-4482-eidd-2801-from-cytidine.pdfDirect link to full text PDF
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YesWhether a free full text is available
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goldOpen access status per OpenAlex
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https://chemrxiv.org/engage/api-gateway/chemrxiv/assets/orp/resource/item/60c754ff9abda2432ff8e284/original/progress-towards-a-large-scale-synthesis-of-molnupiravir-mk-4482-eidd-2801-from-cytidine.pdfDirect OA link when available
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Transamination, Yield (engineering), Cytidine, Chemistry, Drug, Combinatorial chemistry, Pharmacology, Medicine, Enzyme, Biochemistry, Materials science, MetallurgyTop concepts (fields/topics) attached by OpenAlex
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0Total citation count in OpenAlex
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10Number of works referenced by this work
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10Other works algorithmically related by OpenAlex
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| abstract_inverted_index.<p>Molnupiravir | 3 |
| cited_by_percentile_year | |
| countries_distinct_count | 1 |
| institutions_distinct_count | 9 |
| sustainable_development_goals[0].id | https://metadata.un.org/sdg/3 |
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| sustainable_development_goals[0].display_name | Good health and well-being |
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| citation_normalized_percentile.is_in_top_10_percent | False |