Abstract: In the past decade, thousands of chiral organocatalysts have emerged for asymmetric synthesis, and opened up new channels and shortcuts, especially in the synthesis of chiral drug intermediates. They play an important role in developing new methods for the synthesis of new drugs. In these review, chiral organocatalytic reactions are summarized and classified based on the interaction manner way between chiral organocayalysts and substrates. The latest developments of organocatalysis and their applications in drug synthesis are present hereinafter for exploring and developing better organocatalysis.