Free Amino Group Transfer via α‐Amination of Native Carbonyls

Abstract We report herein a straightforward transfer of a free amino group (NH 2 ) from a commercially available nitrogen source to unfunctionalized, native carbonyls (amides and ketones) resulting in direct α‐amination. Primary α‐amino carbonyls are readily produced under mild conditions, further enabling diverse in situ functionalization reactions—including peptide coupling and Pictet–Spengler cyclization—that capitalize on the presence of the unprotected primary amine.