Organic Chemistry Portal



Pd-Catalyzed Indole Synthesis via C-H Activation and Bisamination Sequence with Diaziridinone

Jianjun Wang, Xiaofeng Sun, Daguo Hu and Yian Shi*

*Institute of Natural and Sythetic Organic Chemistry, Changzhou University, Changzhou 213164, China, Email:

J.-W. Ren, M.-N. Tong, Y.-F. Zhao, F. Ni, Org. Lett., 2021, 23, 7497-7502.

DOI: 10.1021/acs.orglett.1c02757

see article for more reactions


A wide variety of indoles can be obtained in good yields from readily available vinyl bromides and diaziridinone. The Pd-catalyzed reaction likely proceeds through a sequential aryl C-H activation and bisamination of a resulting pallada(II)cycle.

see article for more examples

synthesis of bioactive indoles

proposed mechanism

Key Words


ID: J54-Y2021