Asymmetric N-Allylation of Indoles Through the Iridium-Catalyzed Allylic Alkylation/Oxidation of Indolines


  • We thank the National Basic Research Program of China (973 Program 2010CB833300) and the NSFC (20923005, 20932008, 21025209, and 21121062) for financial support. We also thank Prof. Dr. G. Helmchen of Univ. Heidelberg for generously offering dbcot.


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Two steps can be better than one: An efficient synthesis of enantioenriched N-allylindoles by a one-pot Ir-catalyzed asymmetric allylic alkylation/oxidation reaction of indolines has been realized. The current method features high regioselectivity and enantioselectivity together with a broad range of indoles with varying electronic properties. The utility of this method was demonstrated by the synthesis of dihydropyrrolo[1,2-a]indole derivatives.