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. The multicomponent strategy utilizes primary aliphatic amines as C-C-N synthons, aromatic aldehydes as the C1 synthon and ammonium iodide as the nitrogen source. Notably, this transformation achieves α-C(sp3)-H and β-C(sp3)-H bonds functionalization of primary aliphatic amines in one-pot, concurrently forming one C-C bond and three C-N bonds. This method offers a valuable alternative for synthesizing structurally diverse pyrimidines.