Quinoxaline has become a subject of extensive research due to its emergence as an important chemical moiety, demonstrating a wide range of physicochemical and biological activities. The last few decades have witnessed several publications utilizing quinoxaline scaffolds for the design and development of numerous bioactive molecules, dyes, fluorescent materials, electroluminescent materials and organic sensitizers for solar cell applications and polymeric optoelectronic materials. Therefore, to fulfill the need of the scientific community, tremendous effort has been observed in the development of newer synthetic strategies as well as novel methodologies to decorate the quinoxaline scaffold with proper functional groups. Hence, to provide an updated comprehensive account of the diverse synthetic routes to access quinoxaline as well as approaches for structural diversifications, we have attempted to document the synthetic strategies and their functionalization with possible mechanistic rationalization. This will no doubt be helpful for the readers who are anticipating a comprehensive overview on quinoxaline as well as benefitting researchers for future development.