The Pharmaceutical Roundtable of the American Chemical Society's Green Chemistry Institute has deemed cross-couplings that avoid haloaromatics one of their top aspirational reactions. With the support of the Pharmaceutical Roundtable and an NSF-GOALI grant, Michigan State University and Merck have teamed up to advance Ir-catalyzed C�H borylations and eliminate the need for halogens in both electrophilic and nucleophilic cross-coupling partners. Herein, we will describe how through the use of high throughput experimentation, we gained a deeper understanding of how various catalysts, ligands, and other experimental conditions affect Ir-catalyzed C�H borylations. We will also describe how novel manipulation of the borylated products afforded by these reactions can enable the green synthesis unique cross-coupling substrates that are of pharmaceutical interest.

Meeting the aspirations of the ACS/GCI's pharmaceutical roundtable through an academic-industrial collaboration aimed at advancing catalytic borylations

246th National Meeting (2013)

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