Development of a Robust, Green, and Scalable Process for the Synthesis of Fluorobenzene Derivatives from Substituted Diazonium Tetrafluoroborates

Despite the pivotal role of fluorine in modern drug discovery, conventional syntheses of fluorobenzene derivatives suffer from limitations such as harsh conditions, hazardous by-products, and poor functional group tolerance. To address these challenges, we report a robust, green, and scalable process starting from substituted diazonium tetrafluoroborates. Our method has higher security, operates in an anhydrous system to minimize corrosion, and enables the recovery and reuse of both HF and generated fluoroboric acid, while avoiding BF₃ formation. This practical protocol delivers superior yields for a broad range of fluorobenzene derivatives, offering an efficient and sustainable alternative for pharmaceutical and fine chemical synthesis.