A method for the direct methylation of aryl, heteroaryl, and vinyl boronate esters is reported, involving the reaction of iodomethane with aryl-, heteroaryl-, and vinylboronate esters catalyzed by palladium and PtBu<sub>2</sub>Me. This transformation occurs with a remarkably broad scope and is suitable for late-stage derivatization of biologically active compounds via the boronate esters. The unique capabilities of this method are demonstrated by combining carbon-boron bond-forming reactions with palladium-catalyzed methylation in a tandem transformation.
Lucy van Dijk, Brittany C. Haas, Ngiap‐Kie Lim, Kyle Clagg, Jordan J. Dotson, Sean M. Treacy, Katarzyna A. Piechowicz, Vladislav A. Roytman, Haiming Zhang, Dean Toste, Scott J. Miller, Francis Gosselin, Matthew S. Sigman
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