Rhodium(III)-Catalyzed Regioselective C4 Alkylation of Indoles with Nitroalkenes

J Org Chem. 2024 Dec 6;89(23):17844-17849. doi: 10.1021/acs.joc.4c02236. Epub 2024 Nov 20.

Abstract

The Rh(III)-catalyzed indole C4-H bond addition to nitroalkenes is disclosed under mild and redox-neutral reaction conditions, offering straightforward access to various 4-(2-nitroalkyl)indoles (34 examples) with excellent chemo- and regioselectivity. Furthermore, late-stage diversifications and mechanistic studies were also performed.