Palladium-Catalyzed Dearomative Heck/C-H Activation/[4 + 2] Decarboxylative Cyclization of C2-Tethered Indoles
Liwei Zhou1,2, Rui Liu2, Shuyi Guo2
1Hunan Provincial Key Laboratory of the TCM Agricultural Biogenomics, College of Pharmacy, Changsha Medical University, Changsha, Hunan 410219, China.
None:
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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