Abstract The use of ligands to tune the reactivity and selectivity of transition metal catalysts for C (sp 3)–H bond functionalization is a central challenge in synthetic organic chemistry. Herein, we report a rare example of catalyst-controlled C (sp 3)–H arylation using pyridine and quinoline derivatives: The former promotes exclusive monoarylation, whereas the latter activates the catalyst further to achieve diarylation. Successive application of these ...