The secondary metabolites present in medicinal orchids are diverse and possess a vast array of biological activities. They represent valuable raw materials for modern pharmaceuticals and clinical medicine and have tremendous potential for future development. A systematic collation of secondary metabolites’ composition and a summary of the biological activities of medicinal orchids represent a crucial step in unlocking the potential of these valuable resources in drug development. Furthermore, such information can provide essential guidance for comprehensively analyzing the pharmacological and therapeutic mechanisms of these valuable herbs in traditional Chinese herbal medicine. This review article presents an overview of the types and main biological functions of the secondary metabolites found in medicinal orchids, as well as the conventional synthesis methods for these compounds. Our aim is to provide a useful reference for future research and the drug development of secondary metabolic products of medicinal orchids.