Huiying Niu

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It is important to achieve diverse functionalization of tertiary anilines due to its importance in biological molecules, pharmaceutical, function materials, ligands. A straightforward Pd/Cu-catalyzed oxidative C-H bond activation/N-dealkylative carbonylation of tertiary [1, 1'-biphenyl]-2-anilines towards the synthesis of various biologically important phenanthridin-6(5H)-ones has been developed. A wide range of functional groups are well tolerated in this transformation.

Recently, utilizing CO as a methylation reagent to construct functional chemicals has attracted significant attention. However, the conversion of CO is still a challenge due to its inherent inertness. In this study, we have developed a catalyst-free N-methylation of amines to prepare numerous methylamines using CO as a methyl source. By utilizing 2 eq. PhSiH as the reductant, amines could undergo N-methylation under 1 atm of CO in DMF at 90 °C.