Palladium-catalyzed intermolecular amination of unactivated C(sp3)–H bonds was developed. Using NFSI as both the amino source and the oxidant, this protocol operates under mild conditions with excellent terminal selectivity and a broad substrate scope. Moreover, the directing group can be easily removed to produce 1,2-amino alcohols.

•Pyrimidine ring shows a wide variety of pharmacological properties.•6-Oxo-1,4,5,6-tetrahydropyrimidine compounds were found to be a new class of potential anti-influenza agents.•Evaluate their ability of inhibiting neuraminidase (NA) of influenza A virus.•Compound 6g exhibited the strongest inhibitory activity against influenza virus A NA (IC50 = 17.64 μM).•Molecular modeling was applied to illustrate compound interactive with proteins.A series of 6-oxo-1,4,5,6-tetrahydropyrimidine-5-carboxylate derivatives were prepared to evaluate their ability of inhibiting neuraminidase (NA) of influenza A virus. All the compounds were synthesized in good yields starting from aldehyde by using a suitable synthetic strategy, which showed moderate inhibitory activity against influenza A NA. Compound 6g exhibited the strongest inhibitory activity against influenza virus A NA (IC50 = 17.64 μM), which indicated pyrimidine ring could be used as a core structure to design novel influenza NA inhibitors.A series of 6-oxo-1,4,5,6-tetrahydropyrimidine-5-carboxylate derivatives were prepared. Most of them have moderate NA inhibitory activity which indicated pyrimidine ring could be used as a core structure to design novel influenza NA inhibitors.

[Fe(N4Py)(CH3CN)](ClO4)2 can efficiently catalyze intermolecular nitrene insertion of sp3 C–H bonds with bromamine-T as the nitrene source, forming the desired tosylprotected amines with NaBr as the by-product.

Palladium-catalyzed intermolecular amination of unactivated C(sp3)–H bonds was developed. Using NFSI as both the amino source and the oxidant, this protocol operates under mild conditions with excellent terminal selectivity and a broad substrate scope. Moreover, the directing group can be easily removed to produce 1,2-amino alcohols.