SiliaCat diphenylphosphine palladium(II) catalyzed borylation of aryl halides

We investigate the heterogeneously catalyzed direct synthesis of boronic acid pinacol esters using a wide range of aryl chlorides, bromides, and iodides, and bis(pinacolato)diboron as the borylating agent over the sol-gel entrapped SiliaCat diphenylphosphine palladium(II) catalyst. Optimization of the reaction conditions, scale-up of the optimized process, and analysis of palladium leaching enabled us to establish a new selective route for direct access to a diverse set of boronic acid pinacol esters. Clean borylation for scale-up: With the easy access and broad availability of diverse borylated species, the Suzuki-Miyaura reaction has become routine in industry and in research labs. We report a new selective route for direct access to a diverse set of boronic acid pinacol esters over the sol-gel entrapped SiliaCat diphenylphosphine palladium(II) catalyst that can be easily scaled-up. © 2014 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.