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  • Title: Facile synthesis of 1,2,3,4-tetrahydro-beta-carbolines by one-pot domino three-component indole formation and nucleophilic cyclization.
    Author: Ohta Y, Oishi S, Fujii N, Ohno H.
    Journal: Org Lett; 2009 May 07; 11(9):1979-82. PubMed ID: 19354232.
    Abstract:
    Two direct synthetic methods of 1,2,3,4-tetrahydro-beta-carboline derivatives have been developed. After initial indole formation by copper-catalyzed domino three-component coupling-cyclization using an appropriate ethynylaniline, aldehyde, and a secondary amine, treatment with t-BuOK/hexane or MsOH afforded the desired tetrahydro-beta-carboline derivatives in moderate to good yields.
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