A 1-pot synthesis of the SARS-CoV-2 Mpro Inhibitor Nirmatrelvir, the key ingredient in Paxlovid

14 September 2022, Version 1
This content is a preprint and has not undergone peer review at the time of posting.

Abstract

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 53%.

Supplementary materials

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Supporting Information
Description
Optimization of reaction protocols and NMR, HRMS, and HPLC data of isolated compounds.
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