Rh(III)-catalyzed selective mono- and dual C-H bond functionalization of N-aryl benzamidines with iodonium ylides.

A Rh(III)-catalyzed selective mono- and dual C-H bond functionalization reaction of N-aryl benzamidines with iodonium ylides has been developed. Notably, this process enables unprecedented site-selective C-H activation solely on the N-aryl ring of N-arylbenzamidine scaffolds. The reaction shows remarkable selectivity depending on the reaction time and stoichiometry of iodonium ylides, providing a facile divergent route to access both mono- and dual functionalized N-aryl benzamidine derivatives. This synthetic protocol exhibits wide substrate compatibility, is feasible for gram-scale preparation, and allows for further structural modification.