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Palladium-Catalyzed Dearomative Heck/C-H Activation/[4 + 2] Decarboxylative Cyclization of C2-Tethered Indoles. | LitMetric

Palladium-Catalyzed Dearomative Heck/C-H Activation/[4 + 2] Decarboxylative Cyclization of C2-Tethered Indoles.

J Org Chem

Key Laboratory of Chemical Biology and Traditional Chinese Medicine Research (Ministry of Education), and Key Laboratory of the Assembly and Application of Organic Functional Molecules of Hunan Province, College of Chemistry and Chemical Engineering, Hunan Normal University, Changsha, Hunan 410081,

Published: September 2025


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Article Abstract

We herein report a palladium-catalyzed dearomative Heck/C(sp)-H activation/[4 + 2] decarboxylative cyclization of C2-tethered indoles. In this transformation, the alkylpalladium(II) species generated by indole dearomatization undergoes C-H activation to form ,-palladacycles, which are subsequently trapped by -bromobenzoic acids or cyclic β-bromoacrylic acids, enabling regio- and diastereoselective construction of hexacyclic and octocyclic fused indolines with a broad substrate scope.

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Source
http://dx.doi.org/10.1021/acs.joc.5c01929DOI Listing

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