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Updated: Jun 5, 2025

Synthesis of a Borylated Ibuprofen Derivative Through Suzuki Cross-Coupling and Alkene Boracarboxylation Reactions
Published on: November 30, 2022
Palladium-Catalyzed Dual-Tasked ortho-C-H Borylation of Aryl Iodides
Shuai Yang1,2, Fanyi Meng1, Yanghui Zhang1
1School of Chemical Science and Engineering, Shanghai Key Laboratory of Chemical Assessment and Sustainability, Tongji University, Shanghai 200092, People's Republic of China.
Abstract:
The Pd-catalyzed ortho-C-H borylation of aryl iodides has been developed through maleimide-relayed C-H activation. In this reaction, the ipso-positions and ortho-C-H bonds of aryl iodides are alkylated and borylated, respectively, providing a new strategy for C-H borylation. The reaction exhibits a broad substrate scope and represents a modular synthetic method for functionalized 3-aryl succinimides, which are essential structural motifs in organic compounds with diverse biological activities. Furthermore, the boronate group can be further manipulated, and the practical utility of the reaction has been demonstrated. This work also introduces a new strategy for ipso, ortho-difunctionalization of aryl halides via C-H activation.
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