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Enantioselective Borylative Dearomatization of Indoles through Copper(I) Catalysis
Authors:Koji Kubota  Keiichi Hayama  Hiroaki Iwamoto  Prof. Dr. Hajime Ito
Affiliation:Division of Chemical Process Engineering, Graduate School of Engineering, Hokkaido University, Kita 13 Nishi 8 Kita‐ku, Sapporo, Hokkaido 060‐8628 (Japan)
Abstract:The enantioselective borylative dearomatization of a heteroaromatic compound has been achieved using a copper(I) catalyst and a diboron reagent. This reaction involves the regio‐ and enantioselective addition of active borylcopper(I) species to indole‐2‐carboxylates, followed by the diastereoselective protonation of the resulting copper(I) enolate to give the corresponding chiral indolines, which bear consecutive stereogenic centers.
Keywords:borylation  copper  dearomatization  enantioselective synthesis  indoles
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