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Efficient and Versatile Synthesis of Indoles from Enamines and Imines by Cross-Dehydrogenative Coupling

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  • We thank the Alexander von Humboldt Foundation (Z.S.), the European Research Council (ERC) under the European Community’s Seventh Framework Program (FP7 2007-2013)/ERC grant agreement no. 25936, and the Alfried Krupp von Bohlen und Halbach Foundation for generous financial support.

Abstract

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Complement for Fischer: An efficient palladium-catalyzed indole synthesis proceeds by the intramolecular cross-dehydrogenative coupling of N-aryl imines under mild conditions using molecular oxygen as the sole oxidant. This practical method relies on anilines and ketones as starting materials (and thus the same retrosynthetic disconnection as the Fischer indole synthesis) and will likely become a popular route.

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