Chemistry for the Incorporation of S-Aryl Dithiocarbamates into a DNA-Encoded Library

To enable the efficient incorporation of S-aryl dithiocarbamates into DNA-encoded libraries (DELs), we have developed a robust, sequential three-component copper-promoted C(sp²)-S coupling reaction. This protocol employs DNA-conjugated secondary amines, carbon disulfide (CS₂), and commercially available aryl boronic acids as readily accessible substrates, affording structurally diverse DNA-conjugated S-aryl dithiocarbamates, motifs that constitute privileged scaffolds in medicinal chemistry and are recurrent in bioactive compounds.