Synthesis of Densely Substituted Pyrimidine Derivatives

The direct condensation of cyanic acid derivatives with N-vinyl/aryl amides affords the corresponding C4-hetcroatom substituted pyrimidines. The use of cyanic bromide and thiocynatomethane in this chemistry provides versatile azaheterocycles poised for further derivatization. The synthesis of a variety of previously inaccessible C2- and C4-pyrimidine derivatives using this methodology is described.