A 1-Pot Synthesis of the SARS-CoV-2 M pro Inhibitor Nirmatrelvir, the Key Ingredient in Paxlovid.
Juan C CaravezKarthik S IyerRahul D KavtheJoseph R A KincaidBruce H LipshutzPublished in: Organic letters (2022)
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%.