Access to 1-amino-3,4-dihydroisoquinolines via palladium-catalyzed C-H bond aminoimidoylation reaction from functionalized isocyanides.

Efficient access to 1-amino-3,4-dihydroisoquinolines, through palladium-catalyzed intramolecular C-H bond aminoimidoylation of α-benzyl-α-isocyanoacetates, has been developed. Consecutive isocyanide insertion and C-H bond activation were realized with C-N and C-C bonds formation in one step under redox neutral conditions, employing O -benzoyl hydroxylamines as electrophilic amino sources.