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

14 September 2022, Version 1
Working Paper
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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Description
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Supporting Information
Description
Optimization of reaction protocols and NMR, HRMS, and HPLC data of isolated compounds.
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Version History

Sep 14, 2022 Version 1

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The content is available under CC BY 4.0 [opens in a new tab]

DOI

10.26434/chemrxiv-2022-xz3tv
D O I: 10.26434/chemrxiv-2022-xz3tv [opens in a new tab]

Funding

Bill and Melinda Gates Foundation

Author’s competing interest statement

The author(s) have declared they have no conflict of interest with regard to this content

Ethics

The author(s) have declared ethics committee/IRB approval is not relevant to this content

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