DMDM Hydantoin as C1 Precursor for Solvent-Controlled C-3 Hydroxymethylation and Methylenation of Imidazo[1,2-a]pyridines

Abstract

A facile solvent-controlled selective hydroxymethylation and methylenation of imidazo[1,2-a]pyridines using DMDM hydantoin as a C1 source under mild conditions has been developed. The reaction yielded good-to-excellent yields for various imidazo[1,2-a]pyridine derivatives. The key features of this protocol are metal-free, oxidant-free, and operational simplicity. Further modification of the hydroxymethyl group was demonstrated, enabling the synthesis of structurally diverse imidazo[1,2-a]pyridine frameworks. © 2026 Wiley-VCH GmbH.