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  • A Practical Synthesis of In...
    Vaswani, Rishi G; Albrecht, Brian K; Audia, James E; Côté, Alexandre; Dakin, Les A; Duplessis, Martin; Gehling, Victor S; Harmange, Jean-Christophe; Hewitt, Michael C; Leblanc, Yves; Nasveschuk, Christopher G; Taylor, Alexander M

    Organic letters, 08/2014, Letnik: 16, Številka: 16
    Journal Article

    A method for the synthesis of N-functionalized C2-/C3-substituted indoles via Pd-catalyzed C–N bond coupling of halo-aryl enamines is described. The general strategy utilizes a variety of amines and β-keto esters which are elaborated into halo-aryl enamines as latent precursors to indoles. The preferred conditions comprising the RuPhos precatalyst and RuPhos in the presence of NaOMe in 1,4-dioxane tolerate a variety of substituents and are scalable for the construction of indoles in multigram quantities.