Copper-catalysed direct C-H bond sulfonylation of aminoquinolines using commercially available and inexpensive arylsulfonyl chlorides as the sulfonylation reagents is described. The reactions took place exclusively at the C5-H position of the quinoline rings and tolerated a wide spectrum of functional groups. Moreover, synthetic transformations of the sulfonylated products led to useful compounds.

A Cu-catalyzed protocol has been developed for the rapid construction of a wide spectrum of structurally interesting spiropyrroline skeletons. This method utilizes readily accessible ketoximes and alkenes as the starting materials and exhibits broad substrate scope and good functional group compatibility. Furthermore, the reaction can be applied for the late-stage modification of bioactive pregnenolone derivatives. The mechanistic investigation suggests that the reactions proceed through a radical process.

An operationally simple, Pd-catalyzed C-H functionalization is described for the synthesis of important and useful isoindolinones from readily available carboxamides and carboxylic acids or anhydrides. The reactions proceed efficiently with a broad range of substrates under redox-neutral reaction conditions and tolerate a diversity of functional groups. The mechanistic investigation suggests that the reactions involve C-H activation, nucleophilic addition, β-O elimination, and dehydration steps.

A useful approach is developed for the synthesis of various structurally interesting spirocyclic sultams and heterobiaryls using a cross-dehydrogenative coupling strategy that features high atom and step economy. This method employs [Cp*RhCl2]2 as a catalyst and N-sulfonylimine, a weak coordinating group, as an efficient directing group to assist C-H activation. A number of the coupled products were converted into interesting molecules through further synthetic transformations.