Synthesis and anti-neuroinflammatory activity studies of substituted 3,4-dihydroquinoxalin-2-amine derivatives

We demonstrate the synthesis of multifunctional 3,4-dihydroquinoxalin-2-amine derivatives 4 through a three-component condensation reactions of a substituted o-phenylenediamines 1 (OPDA), diverse ketones 2 and various isocyanides 3 in the presence of a catalytic amount of p-toluenesulfonic acid (PTSA) affording excellent yields (82-96%) and 10 mol % of silica gel supported sulfuric acid with good yields (85-98%) in ethanol at room temperature (2-4 h). We also carried out the anti-neuroinflammatory activity of 3,4-dihydroquinoxalin-2-amine derivatives and some of the compounds exhibited good activity.

Graphical abstractStructures of 4l and 4n compounds having biological activity.Download full-size image