This note discusses the application of a Minisci-type reaction for the direct alkylation of azoles with carboxylic acids as radical precursors. Different reaction conditions were investigated to achieve high yield of the desired products, focusing on acid strength and solvent screening. Moreover, the reactivity of imidazoles with various carboxylic acids was investigated, showing good yield for most cases. The study reveals the potential of this approach for late-stage functionalization in drug discovery.
Direct Decarboxylative C-2 Alkylation of Azoles through Minisci-Type Coupling
Rosadoni, ElisabettaPrimo
Methodology
;Del Vecchio, AntonioWriting – Original Draft Preparation
;Bellina, Fabio
Ultimo
Supervision
2023-01-01
Abstract
This note discusses the application of a Minisci-type reaction for the direct alkylation of azoles with carboxylic acids as radical precursors. Different reaction conditions were investigated to achieve high yield of the desired products, focusing on acid strength and solvent screening. Moreover, the reactivity of imidazoles with various carboxylic acids was investigated, showing good yield for most cases. The study reveals the potential of this approach for late-stage functionalization in drug discovery.File in questo prodotto:
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