Rapid Methylthiolation of (Hetero)Aryl Halides at Room Temperature Using Sodium Thiomethoxide Via Palladium-Catalysis

We report a Pd-catalyzed strategy for the thiomethylation of (hetero)aryl halides with sodium thiomethoxide at room temperature. The method enables a fast, robust, and scalable thiomethylation protocol that broadly accommodates functional groups, is compat-ible with aqueous environments, and can be translated to methyl isotope-labeling. It was applied to a large variety of substrates, including drugs, unprotected long peptides and proteins.