Pd-Catalyzed Picolinamide-Directed C(sp)-H Sulfonylation of Amino Acids/Peptides with Sodium Sulfinates.

This report describes a Pd-catalyzed picolinamide-directed site-selective C(sp)-H sulfonylation of amino acids and peptides with sodium sulfinates in moderate to good yields. Sulfonylation of levodopa and dopamine drug molecules and late-stage directed peptide sulfonylation are studied for the first time. Broad substrate scope having various functionalities, late-stage drug modifications, and various post synthetic utilities such as chalcogenation, bromination, olefination, and arylation are potential advantages.