Access to polysubstituted pyrimidine derivatives via the aza-Diels–Alder reaction of 1,2,3-triazine derivatives and amidines

Abstract

The synthesis of highly substituted pyrimidine derivatives by the aza-Diels–Alder reaction of 1,2,3-triazines with amidine derivatives is described. This reaction provided direct access to a wide range of 6-aryl-2-substituted pyrimidine-4-carboxylates in good yields with good functional group compatibility. A broad substrate scope, and the operationally simple, metal-free, and neutral reaction conditions are the prominent features of this method.