Gamma-Selective Alkene Hydroarylation with Arylboronic Acids

As part of an ongoing collaboration with Pfizer, today we report a new method for achieving γ-selective hydroarylation of alkenyl carbonyl compounds, which is available as a pre-print on ChemRxiv (click here).  This reaction is notable for its simplicity, practicality, and functional group tolerance. Because of the ubiquity of arylboronic acids in pharma and in academia, this protocol offers a powerful approach to appending an aryl group of one’s choosing to the γ-position of a carboxylic acid substrate. Congrats to all of the authors: Rei, Tanner, Kin, and Rohan from TSRI; and Gary, Shouliang, Mingying, Fen, and Indra from Pfizer. It was great working with the Pfizer team to field-test the method and to identify valuable heterarylboronic acids that would be of interest to medicinal chemists. Special shoutout to high school student co-author, Rohan, who worked with us earlier this year as part of his junior year internship. Great work, team! Stay tuned for the peer-reviewed version.