Abstract
Practical, undirected and selective catalytic functionalization of unactivated arenes remains a challenging problem in organic synthesis. We herein report a bioinspired L-cystine-derived ligand BCPOM/Fe-enabled innate C-H difluoromethylation of unactivated arenes as limiting reagents with stable and inexpensive BrCF2CO2Et as the difluoromethylation source in high efficiency. Notably, this method uses environmentally benign H2O2 as the sole oxidant, and enables late-stage functionalization and exceptionally functional-group tolerance, even including oxidation-labile aldehyde, phenolic hydroxy, primary amine, and boronic acid groups, which is difficult to access by current means.
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