Abstract
We describe a coinage-metal-catalyzed site-selective oxidation of secondary C(sp(3))-H bonds for aliphatic amine substrates. Broad amine scope, good functional compatibility and late-stage diversification are demonstrated with this method. The steric demand of the β-substituents controlled diastereoselectivities under this catalytic system. The site selectivity favors secondary C(sp(3))-H bonds over tertiary ones underscoring the unique synthetic potential of this method.