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Palladium-mediated C–H activation creates fused indolines from C2-tethered indoles, indicating its broad applicability.
We herein report a palladium-catalyzed dearomative Heck/C(sp2)-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 C,C-palladacycles, which are subsequently trapped by o-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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Zhou et al. (2025) studied this question.
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