Development and patent synthesis of nirmatrelvir - the main component of the first oral drug against SARS-CoV-2 Paxlovid (R)

Nirmatrelvir is the main component of the first oral drug against SARS-CoV-2 called Paxlovid (R). Its development from an orally unavailable predecessor through hydrogen bond donors (HBD) replacement is highlighted, followed by an examination of the synthetic routes described in the original PCT application WO2021/250648. Based on its attributes, nirmatrelvir shows the potential to be a game changer in SARS-CoV-2 treatment.