Pyranoflavonoids are mainly distributed in Leguminosae, Moraceae. As a potent drug candidate, pyranoflavonoids have attracted much attention in late years due to their impressive pharmaceutical activities. The structure characteristics, plant resources and pharmaceutical activities of pyranoflavonoids are reviewed in this paper. The fragmentation in mass spectrometry is also discussed for quick identification of these chemicals. Due to the low abundance of this flavonoid sub-class in plants, it is required to find an efficient way to synthesize them. Therefore, an overview of chemical synthesis and biological synthesis is presented in this paper. The information given in this paper will be helpful to know pyranoflavonoids and to be utilized in medicines and nutraceuticals.