A 1‑Pot Synthesis of the SARS-CoV‑2 Mpro Inhibitor Nirmatrelvir, the Key Ingredient in Paxlovid

A newly devised route to the Pfizer drug nirmatrelvir is reported that reduces the overall sequence to a 1-pot process and relies on a commercially available, green coupling reagent, T3P. The overall yield of the targeted material, isolated as its MTBE solvate, is 64%.

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Veröffentlicht in:Organic letters 2022-12, Vol.24 (49), p.9049-9053
Hauptverfasser: Caravez, Juan C., Iyer, Karthik S., Kavthe, Rahul D., Kincaid, Joseph R. A., Lipshutz, Bruce H.
Format: Artikel
Sprache:eng
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Zusammenfassung:A newly devised route to the Pfizer drug nirmatrelvir is reported that reduces the overall sequence to a 1-pot process and relies on a commercially available, green coupling reagent, T3P. The overall yield of the targeted material, isolated as its MTBE solvate, is 64%.
ISSN:1523-7060
1523-7052
DOI:10.1021/acs.orglett.2c03683