The treatment of various pathological conditions in human beings involves the use of safe and efficacious drug substances. But there are different complications associated with the treatment of various disease states including drug resistance, adverse drug reactions, toxicity, etc. To minimize these problems, there is an urgent need to develop new therapeutics with suitable pharmacokinetic and pharmacodynamic properties. So, the organocatalytic methods are emerged as a potential synthetic tool to accelerate the design of new drug candidates with improved physicochemical and pharmacological properties, selectivity, and efficiency for the treatment of life-threatening diseases. Organocatalytic reactions refer to the chemical reaction that is accelerated by organic catalysts instead of using organometallic catalysts. Organocatalysts are more advantageous in comparison to metallic catalysts because organocatalysts are cost-effective, stable, efficient, non-toxic, readily available, and easy to handle. In addition to this, the organocatalysis method involves an eco-friendly reaction by minimizing the formation of by-products and reducing the chemical hazards. Organocatalysts are categorized into four classes such as Lewis acids, Lewis bases, Bronsted acids, and Bronsted bases. These catalysts are generally involved in various reactions mechanisms such as Aldol reaction, Diels–Alder reactions, Michael Addition and Knoevenagal reactions, etc. The utility of organocatalyst in synthetic chemistry results in the development of medicinally active compounds with diverse structural features.