Catalytic Atroposelective C7 Functionalisation of Indolines and Indoles.

Abstract

Axially chiral atropisomeric compounds are widely applied in asymmetric catalysis and medicinal chemistry. In particular, axially chiral indole‐ and indoline‐based frameworks have been recognised as important heterobiaryl classes because they are the core units of bioactive natural alkaloids, chiral ligands and bioactive compounds. Among them, the synthesis of C7‐substituted indole biaryls and the analogous indoline derivatives is particularly challenging, and methods for their efficient synthesis are in high demand. Transition‐metal catalysis is considered one of the most efficient methods to construct atropisomers. Here, we report the enantioselective synthesis of C7‐indolino‐ and C7‐indolo biaryl atropisomers by means of C−H functionalisation catalysed by chiral RhJasCp complexes.