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Synthesis of α-Ketoamides via Gold(I) Carbene Intermediates

Zuo Zuo Wu, Tapas Adak, Martin C. Dietl, Tao Wang, Chao Hu, Hongwei Shi, Petra Krämer, Matthias Rudolph, Frank Röminger, A. Stephen K. Hashmi

2022Organic Letters21 citationsDOI

Abstract

α-Ketoamides have been found to be an important functional group in a broad spectrum of inhibitors such as the Corona virus and other viruses. Here we report an unprecedented gold-catalyzed 2-fold reaction of a bromoalkyne with anthranils. Hydrolysis of the initial product then directly leads to α-ketoamides. Water addition to the intermediate α-iminoimidoyl halides delivered α-ketoamides from a broad range of bromoalkynes.

Topics & Concepts

ChemistryCarbeneBroad spectrumHalideHydrolysisCatalysisCombinatorial chemistryOrganic chemistryCatalytic Alkyne ReactionsCyclopropane Reaction MechanismsSynthetic Organic Chemistry Methods
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