Abstract
We describe here a Cu-catalyzed and 4-OH-TEMPO-mediated sequential dehydrogenation/aza-Michael addition/annulation cascade reaction for the construction of N-alkyl 2-arylindoles from facilely available saturated ketones and 2-arylethynylanilines. This reaction shows high regioselectivity and tolerates a variety of functional groups. Moreover, 3-alkyl-substituted indoles can also be achieved when using 2-alkylethynylanilines as starting materials.
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