An eco-friendly methodology for the synthesis of novel Schiff base analogs of Raltegravir, an integrase inhibitor drug, is described. Thus, pertinence of these imine derivatives is related to Medicinal Chemistry to develop new anti-HIV compounds. Based on thorough search of the relevant literature, this is the first report of the synthesis of Schiff base using a Raltegravir drug fragment as amino component. In addition, these imines will be used as a synthetic precursor to prepare other biologically relevant nitrogen heterocycles, such as 1,5-disubstituted tetrazoles.