3,4-Fused tricyclic indole scaffolds are ubiquitous in bioactive natural products and pharmaceuticals. A new protocol for the synthesis of 3,4-fused tricyclic indoles has been developed through cascade carbopalladation and C–H amination with N,N-di-tert-butyldiaziridinone. The protocol allows access to a range of 3,4-fused tricyclic indoles, including those containing various linkers and fused with medium-sized rings. Rucaparib can be synthesized via this reaction, providing an advantageous synthetic method for the FDA-approved cancer medicine.

A novel and straightforward approach for the synthesis of tribenzo­[b,d,f]­azepines starting from 2-iodobiphenyls and 2-bromoanilines has been developed. A wide range of tribenzo­[b,d,f]­azepines were obtained in good to excellent yields via a cascade intermolecular palladium-catalyzed C–H activation/dual coupling reaction. C,C-palladacycles, which are generated by C–H activation of 2-iodobiphenyls, should be the reaction intermediates.

A method for the synthesis of enantiopure eight-membered nitrogen heterocycles has been developed through diastereoselective cross-coupling of 2-iodobiphenyls with 2-bromobenzylamines. The products represent a novel type of chiral scaffolds, which...