Organocatalysis has emerged as one of the most significant advancements in organic chemistry over the past decades. It relies on small organic molecules as catalysts to accelerate chemical reactions without the use of transition metals. This approach has transformed synthetic strategies, particularly in asymmetric synthesis and the production of enantiomerically pure compounds. The principle of organocatalysis involves activation of reactants through non-covalent interactions such as hydrogen bonding, or through the formation of reactive intermediates like enamines or iminium ions. These activation pathways lower the activation energy, enhance reaction rates, and improve chemo-, regio-, and stereoselectivity. Control over stereochemistry is especially valuable in pharmaceutical synthesis, where the biological activity of a compound often depends on its three-dimensional structure. Major categories of organocatalysis include amine catalysis, Brønsted acid catalysis, and chiral organocatalysis. These catalytic systems have demonstrated high efficiency in carbon–carbon bond formation reactions such as aldol reactions, Michael additions, nucleophilic additions, cyclization processes, and condensation reactions. A key advantage of organocatalysis is its compatibility with green chemistry principles. By eliminating heavy metal catalysts, it reduces environmental contamination and simplifies product purification. Many organocatalysts are relatively stable, non-toxic, and easy to handle, making them attractive for large-scale industrial applications. In industry, organocatalysis is widely used in the synthesis of active pharmaceutical ingredients, fine chemicals, and advanced functional materials. It also provides valuable insight into reaction mechanisms, supporting the rational design of more efficient catalytic systems. Although challenges remain, including catalyst loading optimization and expanding the scope of applicable reactions, organocatalysis continues to grow rapidly and represents a cornerstone of sustainable and innovative organic synthesis.