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Rh(III)-Catalyzed Synthesis of N-Unprotected Indoles from Imidamides and Diazo Ketoesters via C-H Activation and C-C/C-N Bond Cleavage

Zisong Qi, Songjie Yu and Xingwei Li*

*Dalian Institute of Chemical Physics, Chinese Academy of Sciences, Dalian 116023, P. R. China, Email:

Z. Qi, S. Yu, X. Li, Org. Lett., 2016, 18, 700-703.

DOI: 10.1021/acs.orglett.5b03669 (free Supporting Information)


A Rh(III)-catalyzed C-H activation/annulation of imidamides with α-diazo β-ketoesters enables the synthesis of N-unprotected indoles. A rhodacyclic intermediate has been isolated and a plausible mechanism has been proposed.

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ID: J54-Y2016