Synthesis of α-Ketoamides via Gold(I) Carbene Intermediates
2022
Wu, Zuo Zuo | Adak, Tapas | Dietl, Martin C. | Wang, Tao | Hu, Zhao | Shi, Hongwei | Krämer, P. (Petra) | Rudolph, Matthias | Rominger, Frank | Hashmi, A. Stephen K.
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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