A sustainable synthesis of the SARS-CoV-2 Mpro inhibitor | ResearchBunny

Index

Abstract

This paper presents a novel 7-step, 3-pot synthesis of nirmatrelvir, the active ingredient in Paxlovid, achieving a 70% overall yield. The synthesis utilizes green technology, avoiding traditional peptide coupling reagents and epimerization of stereocenters. DFT calculations predict the presence of two rotamers with a high rotational barrier. Comparisons with Pfizer's original method highlight the reduced cost and environmental impact of this new route.

Publisher

Communications Chemistry

Published On

Nov 21, 2022

Authors

Joseph R. A. Kincaid, Juan C. Caravez, Karthik S. Iyer, Rahul D. Kavthe, Nico Fleck, Donald H. Aue, Bruce H. Lipshutz

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