4.7 Article

A Mild Cu(I)-Catalyzed Oxidative Aromatization of Indolines to Indoles

Journal

JOURNAL OF ORGANIC CHEMISTRY
Volume 81, Issue 20, Pages 10009-10015

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/acs.joc.6b01854

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A novel method for the oxidation of indolines to indoles is described. The method uses a Cu(I) catalyst and an organic percarbonate as the stoichiometric oxidant. The procedure was successfully applied at 0.5 kg scale in the production of a key intermediate in the synthesis of Elbasvir, which is a novel therapy for the treatment of hepatitis C virus infection.

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