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

Wu, Zuo Zuo; Adak, Tapas; Dietl, Martin C.; Wang, Tao; Hu, Zhao; Shi, Hongwei; Krämer, P.; Rudolph, Matthias; Rominger, Frank; Hashmi, A. Stephen K.

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

2022

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.

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