The first example of Ir­(III)-catalyzed C–H activation/cyclization with N-alkoxyamides as amidation reagents to simultaneously form functionalized thiadiazine 1-oxide derivatives was developed. This one-pot cascade protocol tolerated diverse functional groups and readily constructed various heterocyclic frameworks in moderate to good yield.

An effective and condition-controlled way to synthesize with high selectivity a variety of functionalized indoles with potent biological properties has been developed. Notably, 2,4-dialkynyl indole products were obtained by direct double CÀ H bond alkynylation, whereas alkynyl at the C4 position could convert to carbonyl to generate 2alkynyl-3,4-diacetyl indoles fast and effectively. Additionally, a one-pot relay catalytic reaction led to 2,5-di-alkynyl-3,4diacetyl indoles when using a carbonyl group as the directing group and by controlling the type and quantity of additives. A possible mechanism was proposed based on many studies including deuterium-exchange experiments, the necessary conditions of product conversion, and the effect of water on the reaction.

The ruthenium-catalyzed remote ε-C–H alkylation of phosphines with tertiary alkyl halides has been developed. This novel PIII-directed C–H activation strategy tolerated various functional groups and delivered a wide variety of modified phosphines with excellent meta-site selectivity. Preliminary mechanistic studies indicated that a PIII-assisted ortho-cyclometalation/remote σ-activation pathway might be involved in this methodology.

Novel and efficient rhodium(iii)-catalyzed C–H bond activation and tandem annulation for the synthesis of structurally complex quinazolines have been successfully developed.