Journal Article Enantioselective Borylative Dearomatization of Indoles through Copper(I) Catalysis

Kubota, Koji  ,  Hayama, Keiichi  ,  Iwamoto, Hiroaki  ,  Ito, Hajime

54 ( 30 )  , pp.8809 - 8813 , 2015-06-20 , Wiley-Blackwell
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.

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