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Positional selectivity control in the C–H bond functionalization of aniline derivatives remains a formidable challenge in synthetic organic chemistry. Owing to the broad utility of these compounds across pharmaceuticals, agrochemicals, and materials science, synthetic tactics enabling para -selective C–H bond functionalization of aniline scaffolds have attracted substantial research interest. This review systematically summarizes and dissects recent advances in para -selective C–H bond functionalization methodologies applicable to primary, secondary, and tertiary anilines, encompassing transformations including alkylation, arylation, alkenylation, borylation, acylation, and allylation. The comprehensive analysis presented herein aims to offer valuable insights and practical guidance for the efficient para C–H bond functionalization of aniline derivatives.
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Liu et al. (2026) studied this question.
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