Chemoenzymatic Multicomponent Synthesis of Nirmatrelvir

Authors

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.

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Supplementary material

Chemoenzymatic Multicomponent Synthesis of Nirmatrelvir
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.