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

ABSTRACT: 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.

SUBMITTER: Haydl AM 

PROVIDER: S-EPMC6827334 | biostudies-literature | 2019 Mar

REPOSITORIES: biostudies-literature