Development of Highly Efficient Synthesis of Organoboron Compounds

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Organoboron compounds are an important class of compounds that have been utilized as synthetic intermediates, functional molecules, functional polymers, 10B carriers for neutron capture therapy, and biologically active compounds. For the synthesis of them, direct borylation of unreactive C-H bonds catalyzed by transition metal complexes is one of the most economical, efficient, elegant, and environmentally benign protocols. We found that Ir-and Pd-catalyzed C-H borylation of arenes heteroarenes, alkenes, and benzylic positions of alkylarenes by bis(pinacolato)diboron or pinacolborane provided aryl-, heteroaryl-alkenyl, and benzylboron compounds, respectively.