Chemoenzymatic Multicomponent Synthesis of Nirmatrelvir

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

Abstract

We report a new synthesis of the Covid-19 drug nirmatrelvir featuring a highly enantioselective biocatalytic desymmetrization and a diastereoselective multicomponent reaction as the key steps. Our route avoids the use of transition metals and peptide coupling reagents, resulting in an overall highly atom-economic process.

Keywords

Covid-19
antiviral
multicomponent reactions
biocatalysis
stereoselective synthesis

Supplementary materials

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Title
Chemoenzymatic Multicomponent Synthesis of Nirmatrelvir
Description
We report a new synthesis of the Covid-19 drug nirmatrelvir featuring a highly enantioselective biocatalytic desymmetrization and a diastereoselective multicomponent reaction as the key steps. Our route avoids the use of transition metals and peptide coupling reagents, resulting in an overall highly atom-economic process.We report a new synthesis of the Covid-19 drug nirmatrelvir featuring a highly enantioselective biocatalytic desymmetrization and a diastereoselective multicomponent reaction as the key steps. Our route avoids the use of transition metals and peptide coupling reagents, resulting in an overall highly atom-economic process.
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