[15N]-Isotopic labeling: a suitable tool to study the reactivity of bis lactams

The unexpected reactivity of 2,5-diketopiperazines under basic conditions, thanks to N-Boc activation, allows access to valuable pharmacological scaffolds, such as original statine derivatives. Toward this transannular rearrangement of activated lactams (TRAL), we report here the study of bis lactam reactivity using [15N]-isotopic labeling.

Graphical abstractThe reactivity of bis lactams is studied by [15N]-isotopic labeling, toward the transannular rearrangement of activated lactams (TRAL), a new reaction allowing access to valuable pharmacological scaffolds.Figure optionsDownload full-size imageDownload as PowerPoint slide