Room-temperature nickel-catalyzed borylation/cyclization for the synthesis of benzoxaboroles and benzodiazaborines

Abstract

Benzoxaboroles and benzodiazaborines are pivotal in medicinal chemistry due to their unique biological activities and potential as therapeutic agents. Herein, we present a room-temperature, nickel-catalyzed borylation protocol for their efficient synthesis. Utilizing an inexpensive nickel catalyst system, this method provides a facile synthetic method for a wide range of target compounds. This cost-effective approach offers a sustainable alternative to traditional palladium-based methods, aligning with green chemistry principles by reducing energy input and enhancing reaction efficiency. In addition to expanding the range of boronic acid derivatives, the developed methodology holds significant promise for advancing applications in drug discovery.