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Palladium-Catalyzed Direct 2-Alkylation of Indoles by Norbornene-Mediated Regioselective Cascade C–H Activation
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Lehrstuhl für Organische Chemie I and Catalysis Research Center (CRC), Technische Universität München, Lichtenbergstrasse 4, 85747 Garching, Germany
J. Am. Chem. Soc., 2011, 133 (33), pp 12990–12993
DOI: 10.1021/ja2055066
Publication Date (Web): August 2, 2011
Copyright © 2011 American Chemical Society
Abstract
A palladium-catalyzed direct 2-alkylation reaction of free N-H indoles has been developed. This reaction relies on a norbornene-mediated cascade C–H activation process at the indole ring, which features high regioselectivity and excellent functional group tolerance. The reaction represents the first example for a generally applicable, direct C–H alkylation of indole at the 2-position.
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History
- Published In Issue August 24, 2011
- Article ASAPAugust 02, 2011
- Received: June 14, 2011
ACS
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