Divergent electrosynthesis of diketopiperazines and amides

Abstract

The development of convenient and practical synthetic strategies for constructing bioactive diketopiperazines (DKPs) and amide scaffolds without metal residues is of great interest in organic synthesis. Herein, we report a straightforward and scalable P(V)/I⁻-co-mediated divergent electrosynthesis of bioactive DKPs and amides from readily available amino acids, coupled with favorable green metrics such as a low E-factor (1.07) and PMI (2.07). Mechanistic studies confirmed that the phosphate ester intermediate formed via anodic oxidation serves as a pivotal species in enabling this divergent electrochemical transformation.