Controlling the site-selectivity in the C-H functionalization of anilines is one of the great challenges in synthetic chemistry. Considering the numerous applications of aniline derivatives in pharmaceuticals, agrochemicals and advanced materials, the para-selective functionalization of these scaffolds has received much attention. Various synthetic methods on the para-selective functionalization of primary, secondary and tertiary anilines, including electrophilic aromatic reactions, nucleophilic aromatic reactions, oxidative addition, radical addition, and carbenoid addition are highlighted in this review.