The article presents a nickel-catalyzed vicinal diborylation method that facilitates the introduction of two different boryl groups onto aromatic rings, aiding in the generation of diverse bioactive analogues. Unlike existing methods, this approach demonstrates modularity, regioselectivity, and high tolerance for various functional groups. The reaction utilizes easily obtainable aryl triflates or chlorides and operates under mild conditions. The research also provides mechanistic insights, revealing an unusual reaction pathway involving dearomatization and boron migration, which may influence future boron-based functionalization techniques.
The introduction of diverse vicinal substituents to readily available precursors in small molecule drug development has been simplified by our novel nickel-catalyzed diborylation method.
Utilizing aryl triflates or chlorides, our reaction demonstrates modular, regioselective, and divergent approaches to creating vicinal difunctionalized arenes with high substrate scope.
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