Overcoming the Limitations of γ- and δ-C-H Arylation of Amines through Ligand Development.

ABSTRACT: L,X-Type transient directing groups (TDGs) based on a reversible imine linkage have emerged as broadly useful tools for C-H activation of ketones and free amines. However, competitive binding interactions among multiple reaction components (TDG itself, substrate, and substrate-TDG adduct) with the palladium catalyst often lead to the formation of multiple unreactive complexes, rendering ligand development extremely challenging. Herein, we report the finding of versatile 2-pyridone ligands that addresses these problems and significantly improves the γ-methylene arylation of alkyl amines, extending the coupling partners to a wide range of medicinally important heteroaryl iodides and even previously unreactive heteroaryl bromides. The combination of an appropriate transient directing group an

SUBMITTER: Chen YQ 

PROVIDER: S-EPMC12316175 | biostudies-literature | 2018 Dec

REPOSITORIES: biostudies-literature