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A Pd-catalyzed trans -selective carbosilylation reaction of alkynes has been developed. The trans -vinylpalladium species, generated through intramolecular syn -carbopalladation of alkynes and subsequent cis - trans isomerization, were captured by hexamethyldisilane to form multisubstituted vinylsilanes. This reaction provides a useful strategy for the stereoselective synthesis of isoquinolinone-containing exocyclic tetrasubstituted vinylsilanes.

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 palladium-catalyzed cross-coupling reaction of 2-alkylphenyl bromides with biphenylene has been developed. The reactions formed eight-membered carbocycles through C(sp 3 )-H activation and the formation of two C-C bonds, and the chiral products were obtained with excellent diastereoselectivity. The reaction provides a new strategy for the construction of eight-membered carbocycles, and the products represent a novel type of chiral scaffold.

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 new palladium-catalyzed C(sp 3 )-H amination reaction has been developed. 1-( tert -Butyl)-2-iodobenzene and its derivatives undergo palladium-catalyzed C-H activation to form palladacycles. The palladacycles are aminated with diaziridinone to form indolines as the final products. The reaction represents a new method for the synthesis of 3,3-disubstituted indolines, which are essential structural motifs in many bioactive compounds and pharmaceutical targets.

The first copper-catalyzed enantioselective propargylation of trialkyl methantricarboxylate with propargylic alcohol derivatives was developed. The tricarboxylate unit in the obtained adducts could be easily transformed into a malonate moiety by treating with in situ generated NaOEt in excellent yield without racemization.