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It was reported a ruthenium-catalyzed ortho-alkynylation of benzoic acids. The reaction was directed by a weakly-coordination carboxyl group, provides a feacile route to the synthesis of ortho-alkynylated derivatives. A rarely example of bis(alkynylation) reaction of C-H bonds was described.

A highly efficient and practical transition-metal-free CsOH/O2 catalyst system was developed for the N-alkylation of amines with alcohols under argon. This strategy was compatible with many alcohols and exhibits excellent functional group tolerance. More significantly, the selective formation of secondary amines was achieved in excellent yields. The detailed mechanistic study gave a clear understanding of the role of base and oxygen in the catalytic cycle.

An easily synthesized and accessible N,O-bidentate auxiliary has been developed for selective C-H activation under palladium catalysis. The novel auxiliary showed its first powerful application in C-H functionalization of remote positions. Both C(sp(2))-H and C(sp(3))-H bonds at δ- and e-positions were effectively activated, thus giving tetrahydroquinolines, benzomorpholines, pyrrolidines, and indolines in moderate to excellent yields by palladium-catalyzed intramolecular C-H amination.

Conditions for the ortho-selective trimethylsilylation of oxalyl amide protected benzylamine and phenylethylamine derivatives are developed which tolerate a diverse range of functional groups.

The first Pd-catalyzed regioselective γ-carbonylation of oxalyl amide protected aliphatic amines with carbon monoxide results in the formation of pyrrolidones.

Palladium-catalyzed oxalyl amide directed ortho-alkynylation of arylalkylamine derivatives is reported for the first time. A wide variety of β-arylethamine and γ-arylpropamine derivatives are compatible with this protocol. This method provides a general means to synthesize substituted alkynylarylalkylamine derivatives, highlighting the ability of oxalyl amide in promoting C–H functionalization at unique δ and e positions.

A highly efficient and practical transition-metal-free CsOH/O2 catalyst system is developed for the N-alkylation of amines with alcohols.

An oxalamide derived N,O-bidentate auxiliary is developed to offer the synthesis of various 5- and 6-membered nitrogen heterocycles.