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While late\u2010stage modifications exist for many types of structural features, methods for introducing amines into peptides via a late\u2010stage approach are rare, despite their enormous potential for the development of peptide therapeutics. Here we present a protocol for introducing amines into peptides by our established on\u2010resin iodination\u2010substitution approach. Our method is compatible with a wide variety of amines, including primary and secondary amines, anilines, and other heteroaromatic\n                    <jats:italic>N<\/jats:italic>\n                    \u2010nucleophiles mostly giving good to excellent yields. We introduce amines that are pharmacologically relevant as well as those that can impart catalytic or metal\u2010binding properties into the peptide of interest. As a proof\u2010of\u2010concept study, we introduce the metal ligand tris(2\u2010aminoethyl)amine (tren) into a tryptophan zipper scaffold using our late\u2010stage amination approach to explore metal\u2010induced stapling. Indeed, metal complexation via the tren ligand resulted in a thermal stabilization of more than 30\u00a0K in one of our tryptophan zipper designs.\n                  <\/jats:p>","DOI":"10.1002\/chem.202501229","type":"journal-article","created":{"date-parts":[[2025,5,5]],"date-time":"2025-05-05T06:19:01Z","timestamp":1746425941000},"update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":5,"title":["Late\u2010Stage Amination of Peptides on the Solid Phase"],"prefix":"10.1002","volume":"31","author":[{"ORCID":"https:\/\/orcid.org\/0009-0002-5722-6783","authenticated-orcid":false,"given":"Julian","family":"Brinkhofer","sequence":"first","affiliation":[{"name":"Institute of Organic Chemistry Heidelberg University  Im Neuenheimer Feld 270 69120 Heidelberg 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