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Updated: Mar 13, 2026

A Microwave-Assisted Direct Heteroarylation of Ketones Using Transition Metal Catalysis
Published on: February 16, 2020
Ambient Decarboxylative Arylation of Malonate Half-Esters via Oxidative Catalysis
Patrick J Moon1, Shengkang Yin1, Rylan J Lundgren1
1Department of Chemistry, University of Alberta , Edmonton, Alberta T6G 2G2, Canada.
Abstract:
We report decarboxylative carbonyl α-arylation by coupling of arylboron nucleophiles with malonic acid derivatives. This process is enabled by the merger of aerobic oxidative Cu catalysis with decarboxylative enolate interception reminiscent of malonyl-CoA reactivity in polyketide biosynthesis. This method enables the synthesis of monoaryl acetate derivatives containing electrophilic functional groups that are incompatible with existing α-arylation reactivity paradigms. The utility of the reaction is demonstrated in drug intermediate synthesis and late-stage functionalization.
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