Synfacts 2011(8): 0829-0829  
DOI: 10.1055/s-0030-1260853
Synthesis of Heterocycles
© Georg Thieme Verlag Stuttgart ˙ New York

Heteroannulation Route to Indoles from N-Aryl Enamines via C-H Activation

Contributor(s): Victor Snieckus, Matthew O. Kitching
J. J. Neumann, S. Rakshit, T. Dröge, S. Würtz, F. Glorius*
Bayer CropScience AG, Monheim am Rhein, Westfälische Wilhelms-Universität Münster and Archimica GmbH, Frankfurt am Main, Germany
Further Information

Publication History

Publication Date:
20 July 2011 (online)


Reported is the preparation of indoles 2 from their corresponding N-aryl enamines 1 via an oxidative transition-metal-mediated coupling employing C-H activation. The authors excellently document the broad substrate scope, ­illustrating a wide tolerance of functional groups and variation in the substitution of the aniline ring with ortho and para substitution of the aniline appearing to be particularly well suited to this process. In addition, the process appears to be readily scalable, as well as its conversion into a one-pot process in which the enamine is formed from the aniline component without isolation.