The synthesis of a 5, 7-dichloropyrido [4, 3-d] pyrimidine scaffold is described. The chlorine at position 5 can selectively be displaced by different palladium-catalyzed cross-coupling reactions and nucleophilic aromatic substitutions. In the subsequent step, the chlorine at position 7 can be further derivatized. The described synthetic sequence allows for the construction of a diverse pyrido [4, 3-d] pyrimidine library with structural variations at ...