Site‐Selective Distal C(sp3)−H Bromination of Aliphatic Amines as a Gateway for Forging Nitrogen‐Containing sp3 Architectures

Abstract Herein, we disclose a new strategy that rapidly and reliably incorporates bromine atoms at distal, secondary C(sp 3 )−H sites in aliphatic amines with an excellent and predictable site‐selectivity pattern. The resulting halogenated building blocks serve as versatile linchpins to enable a series of carbon‐carbon and carbon‐heteroatom bond‐formations at remote C(sp 3 ) sites, thus offering a new modular and unified platform that expediates the access to advanced sp 3 architectures possessing valuable nitrogen‐containing saturated heterocycles of interest in medicinal chemistry settings.