Pd-Catalyzed Picolinamide-Directed C(sp2)-H Sulfonylation of Amino Acids/Peptides with Sodium Sulfinates

This report describes a Pd-catalyzed picolinamide-directed site-selective C(sp2)-H sulfonylation of amino acids and peptides with sodium sulfinate in moderate to good yields. Sulfonylation of levodopa and dopamine drug molecules and late-stage di-rected peptide sulfonylation are studied for the first time. Broad substrate scope having various functionalities, late-stage drug modifications, various post synthetic utilities such as chalcogenation, bromination, olefination, and arylation are potential ad-vantages.