Due to the structural characteristics of isoflavones is determined by its poor solubility (fat soluble and water soluble), drug oral bioavailability is low, so the dissolved by structure modification to improve its performance and pharmacological activities has become a research hotspot. At present，the Prodrug principle and combination principles of isoflavones in sites with active group in order to improve the efficacy has made certain achievements, not only to improve the solubility, and the partial derivatives of pharmacological activity is better than that of matrix.In this paper, the current domestic and international acetoxylation of isoflavones, etherification, esterification and halogenated structure modification research status are reviewed, so as to provide reference for further research and development of this compound.