Rapid synthesis of 1,6-naphthyridines by grindstone chemistry

Abstract

Many methods to prepare heterocyclic compounds involve toxic solvents and reagents. There is therefore a need to design cleaner synthetic procedures. 1,6-Naphthyridine derivatives are used in many applications such as cancer chemotherapy, antibacterials, antivirals and antiproliferatives. Here, we report the solvent-free and catalyst-free synthesis of 1,6-naphthyridine derivatives. Synthesis is done by grinding of 2 mmol of ketones, 2 mmol of malononitrile and 1 mmol of amines in a mortar at room temperature for 5-7 min. 1,2-Dihydro[1,6]-naphthyridine derivatives were obtained in 90-97 % yields.