Development and patent synthesis of nirmatrelvir – the main component of the first oral drug against SARS-CoV-2 Paxlovid®
Bruno A. Cotrim
A and José C. Barros B *
+ Author Affiliations
- Author Affiliations
A Instituto Federal de Educação, Ciência e Tecnologia do Rio de Janeiro, Unidade Rio de Janeiro. Rua Senador Furtado, 121, Laboratório 316, Rio de Janeiro, RJ 20270-021, Brazil.
B Instituto de Química, Universidade Federal do Rio de Janeiro, CT Bloco A, Rio de Janeiro, RJ 21941-909, Brazil.
Australian Journal of Chemistry 75(7) 487-491 https://doi.org/10.1071/CH22104
Submitted: 11 May 2022 Accepted: 6 July 2022 Published: 18 August 2022
© 2022 The Author(s) (or their employer(s)). Published by CSIRO Publishing. This is an open access article distributed under the Creative Commons Attribution 4.0 International License (CC BY)
Abstract
Nirmatrelvir is the main component of the first oral drug against SARS-CoV-2 called Paxlovid®. 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.
Keywords: covid-19, drug development, medicinal chemistry, nirmatrelvir, Paxlovid®, organic synthesis, patent, process chemistry, SARS-CoV-2.
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