title: Asymmetric Synthesis of Optically Active Spirocyclic Indoline Scaffolds through an Enantioselective Reduction of Indoles.
abstract: An enantioselective synthesis of spirocyclic indoline scaffolds was achieved by applying an asymmetric iridium-catalyzed hydrogenation of 3H-indoles. Low catalyst loadings and mild reaction conditions provide a broad range of differently substituted products with excellent yields and enantioselectivities. The developed methodology allows an efficient synthesis of this important spirocyclic structural motif, which is present in numerous biologically active molecules and privileged structures in medicinal chemistry.
authors.affiliation: Institute of Organic Chemistry, RWTH Aachen, Landoltweg 1, 52074, Aachen, Germany), Fax: (+49) 241-809-2665.
authors.forename: Ruediger
authors.initials: R
authors.lastname: Borrmann
authors.affiliation: Institute of Organic Chemistry, RWTH Aachen, Landoltweg 1, 52074, Aachen, Germany), Fax: (+49) 241-809-2665.
authors.forename: Nils
authors.initials: N
authors.lastname: Knop
authors.affiliation: Institute of Organic Chemistry, RWTH Aachen, Landoltweg 1, 52074, Aachen, Germany), Fax: (+49) 241-809-2665.|King Abdullah University of Science and Technology (KAUST), KAUST Catalysis Center (KCC), Thuwal, 23955-6900, Saudi Arabia.
authors.forename: Magnus
authors.initials: M
authors.lastname: Rueping
keywords: asymmetric reduction; indoles; iridium catalysis; pharmacophore; spirocycles