The process proved to be of high value, allowing for the seamless integration of a variety of drugs onto the Dha-backbone, yielding an array of novel amino acid/drug conjugates 38. The mild conditions of our photocatalytic hydroarylation were evidenced by the complete preservation of vulnerable heterocyclic structures, such as those found in pyriproxen, bifonazole, boscalid, and benzbromarone. The successful incorporation of drug scaffolds onto amino acid backbones led us to extend our strategy to the chemical ligation of peptides. We utilized an arylthianthrenium salt derivative of phenylalanine under our standard conditions, which afforded the targeted unnatural dipeptide 47 with excellent chemo-and regioselectivity.