ArticleCommunications chemistry2022
A sustainable synthesis of the SARS-CoV-2 M
Article in Communications chemistry, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 papers.
What it found
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The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
10 citing papers in PubMed.
- In Vitro Assessment of Antiviral Activity of Saikosaponin B2 Against Porcine Epidemic Diarrheal Virus.Viruses · 2026Article
- Ligand-Based Design of Selective Peptidomimetic uPA and TMPRSS2 Inhibitors with Arg Bioisosteres.International journal of molecular sciences · 2024Article
- Multicomponent Synthesis of the SARS-CoV-2 Main Protease Inhibitor Nirmatrelvir.The Journal of organic chemistry · 2023Article
- Synthesis of optically active SARS-CoV-2 Mpro inhibitor drug nirmatrelvir (Paxlovid): an approved treatment of COVID-19.Organic & biomolecular chemistry · 2023Article
- A sustainable, efficient, and potentially cost-effective approach to the antimalarial drug candidate MMV688533.Chemical science · 2023Article
- Development of the Commercial Manufacturing Process for Nirmatrelvir in 17 Months.ACS central science · 2023Article
- Investigation of the Compatibility between Warheads and Peptidomimetic Sequences of Protease Inhibitors-A Comprehensive Reactivity and Selectivity Study.International journal of molecular sciences · 2023Article
- Direct formation of amide/peptide bonds from carboxylic acids: no traditional coupling reagents, 1-pot, and green.Chemical science · 2023Article
- An Efficient and Sustainable Synthesis of the Antimalarial Drug Tafenoquine.ACS sustainable chemistry & engineering · 2022Article
- A 1-Pot Synthesis of the SARS-CoV-2 MOrganic letters · 2022Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
7 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Pfizer's drug for the treatment of patients infected with COVID-19, Paxlovid, contains most notably nirmatrelvir, along with ritonavir. Worldwide demand is projected to be in the hundreds of metric tons per year, to be produced by several generic drug manufacturers. Here we show a 7-step, 3-pot synthesis of the antiviral nirmatrelvir, arriving at the targeted drug in 70% overall yield. Critical amide bond-forming steps utilize new green technology that completely avoids traditional peptide coupling reagents, as well as epimerization of stereocenters. Likewise, dehydration of a primary amide to the corresponding nitrile is performed and avoids use of the Burgess reagent and chlorinated solvents. DFT calculations for various conformers of nirmatrelvir predict that two rotamers about the tertiary amide would be present with an unusually high rotational barrier. Direct comparisons with the original literature procedures highlight both the anticipated decrease in cost and environmental footprint associated with this route, potentially expanding the availability of this important drug worldwide.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the Socratic graph.