Modular arene functionalization by differential 1,2-diborylation.

ABSTRACT: Aromatic rings, also known as arenes, containing two or more adjacent different substituents are ubiquitously found in small-molecule drugs¹. Strategies that can rapidly introduce diverse vicinal substituents to readily available precursors would greatly benefit the generation of analogues of biologically active compounds², which, however, remain challenging to realize so far. The existing approaches for preparing vicinal difunctionalized arenes lack modularity, regioselectivity or generality. Here we report a nickel-catalysed arene vicinal diborylation method that can directly install two chemically differentiated boryl groups in a regioselective and site-selective manner using readily available aryl triflates or chlorides as substrates. This reaction operates under

SUBMITTER: Huo J 

PROVIDER: S-EPMC12404689 | biostudies-literature | 2025 Aug

REPOSITORIES: biostudies-literature