3-Bromo-5-methoxybenzaldehyde, can be used for the synthesis of novel scaffold, that led to the discovery of potent and selective Inhibitors of Dihydrofolate Reductase, used for the treatment of Cryptosporidiosis. It can also be used for the synthesis of Tetrahydrobenzoxepino[2,3,4-ij]isoquinolines derivatives, as Dopamine Receptor ligands.