Multicomponent Synthesis of the SARS-CoV-2 Main Protease Inhibitor Nirmatrelvir

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Abstract

In the wake of the Covid-19 pandemic, it has become clear that global access to efficacious antiviral drugs will be critical to combat future outbreaks of SARS-CoV-2 or related viruses. The orally available SARS-CoV-2 main protease inhibitor nirmatrelvir has proven an effective treatment option for Covid-19, especially in compromised patients. We report a new synthesis of nirmatrelvir featuring a highly enantioselective biocatalytic desymmetrization (>99% ee) and a highly diastereoselective multicomponent reaction (>25:1 dr) as the key steps. Our route avoids the use of transition metals and peptide coupling reagents, resulting in an overall highly efficient and atom-economic process.

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Preschel, H. D., Otte, R. T., Zhuo, Y., Ruscoe, R. E., Burke, A. J., Kellerhals, R., … Ruijter, E. (2023). Multicomponent Synthesis of the SARS-CoV-2 Main Protease Inhibitor Nirmatrelvir. Journal of Organic Chemistry, 88(17), 12565–12571. https://doi.org/10.1021/acs.joc.3c01274

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