Quinoxalines are an important group of N-heterocyclic compounds, which are present in a variety of natural and synthetic compounds possessing physicochemical properties and pharmacological activities. Since the earliest studies, their unique properties have led the chemical community, to embrace the challenge of synthesizing new Quinoxalines. This bioactive moiety can act as a versatile building block intermediate in synthesizing novel heterocyclic scaffolds and is considered as prime focus in medicinal chemistry research. This review aims to highlight the recent synthetic strategies and various routes employed to design and synthesize quinoxalines. Initially, we have discussed the classical methods of synthesis followed by modern methods and green methods, with an overview pertaining to their structure-activity-relationship (SAR). We entrust that, this mini review will offer a broad perspective and insights among the readers in the development of new quinoxalines scaffolds with rich bio-potent applications.