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Open Access Publications from the University of California

Palladium-Catalyzed Methylation of Aryl, Heteroaryl, and Vinyl Boronate Esters.

  • Author(s): Haydl, Alexander M;
  • Hartwig, John F
  • et al.

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 PtBu2Me. 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.

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