A novel and simple t-BuOLi/I₂-mediated synthesis of 1,2,4-trisubstituted imidazoles was developed without transition-metal added. The transition-metal-free strategy tolerated a range of substrates and provided products in moderate to good yields with 100% regioselectivity.

An efficient and simple protocol for N-bromosuccinimide (NBS)-mediated styrenes aziridination using amides as the nitrenoid source has been developed. This aziridination affords desired products in moderate to good yields without using transition metal catalyst under very mild reaction condition.

An efficient one-pot N-alkylation of benzimidazole and benzotriazole from carbonyl compounds and tosylhydrazide has been accomplished via copper powder-catalyzed N—H bond insertion affording N-alkylated products in good yields. The reaction can tolerate a wide range of carbonyl compounds, such as aryl, alkyl, heterocyclic and α,β-unsaturated ketones, and aldehydes.

A novel palladium-catalyzed approach to direct C-3-arylation of 1H-indoles with arylhydrazines using air as the oxidant via CN bond cleavage has been developed. Various substituents are tolerated in this system in moderate to good yields. This reaction could also be compatible with a larger scale. Thus, this strategy using arylhydrazines as arylating reagents provides a powerful method for constructing substituted 3-aryl-1H-indoles.

A facile and efficient protocol for the synthesis of 4-substituted-1H-[1,2,3]triazolo[4,5-c]quinolines through a CuO-promoted tandem cyclization reaction has been developed. This method allows for the construction of two heterocyclic rings in a one-pot reaction of readily available (E)-3-(2-bromoaryl)-1-arylprop-2-en-1-ones and sodium azide without the addition of any additive. A series of triazole-fused N-heterocyclic compounds could be prepared in moderate to good yields.

A novel and efficient approach to the synthesis of 2-substituted benzimidazoles has been developed via CuI/DMEDA-catalyzed coupling reaction and post-cyclization with glacial acetic acid from readily available 2-iodoanilines and amides. This method is suitable for the construction of a variety of benzimidazoles in moderate to good yields under short reaction times.

A new approach to synthesize N-alkylation of azoles by iron(III)-catalyst under solvent-free conditions was developed. The method is broad in scope and highly efficient.

Charcoal impregnated with zinc was able to catalyze the cycloaddition of organic azides and alkynes to provide the corresponding 1,4-disubstituted 1,2,3-triazoles and 1,4,5-trisubstituted 1,2,3-triazoles in good to excellent yields. Noteworthy was that the novel and heterogeneous catalyst was successfully applied in this cycloaddition reaction for the first time and could also be easily recycled.