The production of biaryl derivatives is a synthetically important process in the production of many biologically active molecules. One method of synthesizing biaryl and heterobiaryl scaffolds is the Suzuki coupling. However, the need to pre-functionalize these precursors results in an inefficient production of biaryl compounds. A desirable alternative method is the process of direct arylation. In theory, direct arylation has the potential to be a highly efficient process for the coupling of two aromatic rings. However, in practice, the reaction still requires optimization. Although optimization of the selectivity is still being developed, multiple observations suggesting an electronic trend to selectivity were established. By altering the R-group on carboxylic acids, clear reversals in selectivity were achieved. Further, the foundation for research of the topic has been laid to facilitate future work in the area.

Ligand structure influences direct arylation regioselectivities

247th National Meeting (2014)

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