Abstract

Nitroarenes are fundamental feedstocks in the chemical industry. Their relatively inert C−NO2 bond allows for late‐stage modifications of molecules and exhibits complete orthogonality to the reactivity of C−halogen bond in cross‐coupling reactions. The denitrative functionalization of nitroarenes holds significant appeal due to it avoids the use of aryl halides, thereby simplifying reaction steps and improving atom and step economy. Recent progress in direct denitrative functionalization of nitroarenes includes palladium‐catalyzed denitrative coupling, copper‐catalyzed denitrative coupling, as well as metal‐free one‐pot C−NO2 functionalization. In this review, we provide a concise overview of these advancements, detailing the reaction features and mechanisms. This summary aims to highlight the versatility and efficiency of denitrative functionalization methodologies, offering insights into their potential applications and inspiring further research in this promising area of organic synthesis.

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