Four-component assembly of polysubstituted pyrimidines via dual C(sp3)–H functionalization of primary aliphatic amines

Abstract

An efficient iodine-promoted four-component reaction has been developed for the synthesis of diverse polysubstituted pyrimidines from simple and readily available starting materials under metal-free conditions. The multicomponent strategy innovatively utilizes primary aliphatic amines as C–C–N synthons, aromatic aldehydes as C1 synthons and ammonium iodide as an environmentally benign nitrogen source, achieving α-C(sp³)–H and β-C(sp³)–H bond functionalization of primary aliphatic amines in one pot. This method offers a valuable alternative for synthesizing structurally diverse pyrimidines.