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In this contribution, we provide a comprehensive overview on the C−H activation/functionalization reactions of 1‐aryl‐5‐pyrazolones, in particular, 1‐aryl‐3‐methyl‐1H‐pyrazol‐5(4H)‐ones (edaravones) and their N‐methyl analogues i. e., antipyrines covering the literature since 2013 (the year of the first report). This review summarizes the recent progress in C−H functionalization reactions of 1‐aryl‐5‐pyrazolones...