Direct deaminative functionalization

Abstract

Amines, ubiquitous both in nature and synthetic molecules, have long been regarded as static end points in organic synthesis. Unlocking their potential as distinct reactive handles for molecular editing represents a profound shift in synthetic logic. To address this limitation, direct deaminative functionalization has emerged as a transformative solution. This step-economic strategy revolutionizes synthetic design by converting readily available C–N bonds into valuable C–C and C–heteroatom linkages. Herein, we move beyond the fragmented landscape of isolated reports to establish a unified bond-centric framework. By organizing advances according to the specific bond formed, this Review provides a comprehensive and systematic overview of this rapidly expanding field. We highlight the strategic utility of distinct activation platforms in late-stage functionalization, illustrating their value as practical tools for molecular diversification.