The synthesis of biopinein was carried out by the traditional chalcone closed-loop synthetic route, which requires chemical reagents that have the disadvantage of polluting the environment, reacting under drastic conditions, and consuming large amounts of energy. In addition, the product obtained by the chemical method is a mixture of racemates (R-type, S-type), whereas studies have demonstrated that only (2S)-biopsin is biologically active. Therefore, the chemical synthesis method is not suitable for the mass production of biopines.