One-Step Introduction of Nitrogen-Containing Functional Groups onto Aryl Methyl Ketones: Synthesis of α-Iminoamidines with Tunable Biorelevant Properties.

In this work, we report a straightforward one-step oxidative method for introducing three nitrogen atoms into aryl methyl ketones, yielding α-iminoamidines. Minor changes to the reaction conditions or workup, or subsequent simple transformations, unlock a variety of nitrogen-rich scaffolds. Physicochemical data show tunable basicity and lipophilicity─key traits for medicinal chemistry. The scaffold also supports axial stereoisomerism, adding stereochemical diversity.