title: A Mild Cu(I)-Catalyzed Oxidative Aromatization of Indolines to Indoles.
abstract: 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.
authors.affiliation: Department of Process and Analytical Chemistry, Merck & Co. Inc. , Rahway, New Jersey 07065, United States.
authors.forename: Feng
authors.initials: F
authors.lastname: Peng
authors.affiliation: Department of Process and Analytical Chemistry, Merck & Co. Inc. , Rahway, New Jersey 07065, United States.
authors.forename: Mark
authors.initials: M
authors.lastname: McLaughlin
authors.affiliation: Department of Process and Analytical Chemistry, Merck & Co. Inc. , Rahway, New Jersey 07065, United States.
authors.forename: Yizhou
authors.initials: Y
authors.lastname: Liu
authors.affiliation: Department of Process and Analytical Chemistry, Merck & Co. Inc. , Rahway, New Jersey 07065, United States.
authors.forename: Ian
authors.initials: I
authors.lastname: Mangion
authors.affiliation: Department of Process and Analytical Chemistry, Merck & Co. Inc. , Rahway, New Jersey 07065, United States.
authors.forename: David M
authors.initials: DM
authors.lastname: Tschaen
authors.affiliation: Department of Process and Analytical Chemistry, Merck & Co. Inc. , Rahway, New Jersey 07065, United States.
authors.forename: Yingju
authors.initials: Y
authors.lastname: Xu
mesh_terms: D002384:Catalysis; D003300:Copper / Q000737:chemistry*; D007211:Indoles / Q000737:chemistry*; D010084:Oxidation-Reduction; D013057:Spectrum Analysis / Q000379:methods
chemical_list: D007211:Indoles; D003300:Copper