This review aims to provide a comprehensive report on the quinoline ring with respect to its synthesis, reactivity, and therapeutic values. The reactivity of quinoline for the metal, electrophile, and other reactive counterparts defines the shape of the quinoline pharmacophore, which is an important part of this report; moreover, its spectroscopic characteristics have been included herein with suitable illustration. The quinoline and its derivatives have been presented as well as the general synthetic approaches along with the new developments in the catalytic system; the relevant information is also summarized under the various separate activity classes. The synthesis of heterocyclic scaffolds has been a concern for scientists, so herein we have tried to include the synthetic parameters of quinoline with regard to the important pharmacological aspects.