Ursodeoxycholic acid (UDCA) is a widely used pharmacologically active natural bile acid, which can dissolve cholesterol gallstones and improve liver function in cases of cholestasis. UDCA was originally obtained from the bile of live bears, but environmental and animal welfare concerns have made this source increasingly problematic, and increased demand for alternatives. Today, chemical and enzyme-catalyzed syntheses are often used to produce UDCA. Research hot topics have concentrated on UDCA-related precursors with plentiful sources and affordable prices due to the significance of UDCA in the drug treatment of human cholesterol stones and other associated disorders. In this review, the state of research on the chemical and biological synthesis of UDCA from different materials [cholic acid (CA), chenodeoxycholic acid (CDCA), hyodeoxycholic acid (HDCA), etc.] is summarized and analyzed, to guide and inform future research on commercial UDCA production.