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Methodology for Synthesis of Enantiopure 3,5-Disubstituted Pyrrol-2-ones

Publication at Faculty of Pharmacy in Hradec Králové |
2015

Abstract

A new synthetic route towards chiral 3,5-disubstituted pyrrol-2-ones by starting from amino acids has been developed. The sequence features the conversion of amino acids into their corresponding alkynoic acid derivative followed by a Pd-catalyzed hydrostannylation of the triple bond and Stille cross-coupling reaction.

A series of lactam analogues of antifungal 3-(aryl)-5-hydroxymethyl-2,5-dihydrofuran-2-ones have thus been prepared.