An efficient and convenient copper-catalyzed method has been developed to achieve direct ortho-C-H/N-H annulation to synthesize phenanthridinones with arynes. This method highlights an emerging strategy to transform inert C-H bonds into versatile functional groups in organic synthesis and provides a new way to synthesize phenanthridinone alkaloids efficiently.

An efficient and convenient method has been developed to achieve direct silylation of unactivated remote primary or secondary C(sp)-H bonds to form C-Si bonds with hexamethyldisilane (HMDS). This method highlights the emerging strategy to transform unactivated methyl or methylene into versatile functional groups in organic synthesis and provides a new method to construct functionalized C-Si bonds for synthetic chemistry.

We have developed a novel π−π interaction and dual H-bond concerted control strategy to construct axially chiral naphthylamine heterocycles. With ortho-alkynyl-naphthylamines as the electrophile, indoles and 4-hydroxycoumarins were efficiently employed to construct axially chiral skeletons in good yields and with excellent enantioselectivities (up to 97% enantiomeric excess). Furthermore, the resulting products could be converted to potential squaramides featuring organic catalysts.

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Bioinspired palladium‐catalyzed intramolecular cyclization of amino acid derivatives containing a vinyl iodide moiety by C−H activation enabled rapid access to a wide range of functionalized proline derivatives with an exocyclic olefin. To demonstrate the practicality of this methodology, the functionalized prolines were used as intermediates for the synthesis of several natural products: lucentamycin A, oxotomaymycin, oxoprothracarcin, and barmumycin.

Employing silver/rhodium relay catalysis strategy, an intramolecular electrophilic cyclization and CÀ H activation followed by cascade hydrogenation and reductive amination has been developed. The acylmethylated isoquinoline derivatives could be afforded with broad substrate scope in 23-88% yields, which could be further transformed to the core skeleton of hexahydrodibenzo[a,g] quinolizine as drug-candidates. Moreover, this reaction was achieved in a gram-scale. A reasonable reaction mechanism has been proposed based on a series of control and KIE experiments.

In this paper, we revealed a metal-free and visible light photoinduced method for the rapid construction of spirobi[indene] skeletons, providing a simple and efficient way for easy access to spirobi[indene] scaffolds under mild conditions along with a broad substrate scope and good functional group tolerance.

A novel rhodium-catalyzed asymmetric hydroamination and hydroindolation of keto-vinylidenecyclopropanes has been developed, affording the hydroamination and hydroindolation products in good to excellent yields with outstanding ee values through a new TMM–Rh model complex.