Iridium/Acid Co-Catalyzed Direct Access to Fused Indoles via Transfer Hydrogenative Annulation of Quinolines and 1,2-Diketones

Guangpeng Lu,^†Feng Xie, ^‡Rong Xie,^† Huanfeng Jiang,^† andMin Zhang*^,†

ABSTRACT: Herein, we present an unprecedented iridium/acid co-catalyzed construction of fused indoles via transfer hydrogenative annulation of non-activated quinolines and 1,2-diketones. The products are assembled via initial reduction followed by selective coupling of 1,2-diketones with the N and C8 sites of quinolyl skeleton. The developed synthetic method features operational simplicity, readily available feedstocks, applicable for streamline synthesis of functional molecules, high step and atom efficiency, and generation of water as the byproduct.

Link:https://pubs.acs.org/doi/10.1021/acs.orglett.0c00500