A sustainable synthesis of the SARS-CoV-2 Mpro inhibitor nirmatrelvir, the active ingredient in Paxlovid

Abstract

The antiviral drug nirmatrelvir is the active ingredient in Paxlovid, a SARS-CoV-2 Mpro inhibitor developed by Pfizer, however, its synthetic procedure faces limitations for meeting urgent demand. Here, the authors optimize the key synthetic steps and develop a sustainable route to nirmatrelvir in 7 steps and 3 pots with an overall 70% yield.