Andrographolide is one of the major diterpenoidal active constituents of traditional Chinese medicine. In recent years, pharmacologists and organic chemists found that andrographolide and its derivatives have specific bioactivities and pharmaceutical activities, such as anti-tumor, anti-human immunodeficiency virus (HIV) and α-glucosidase inhibitors. In this paper, the development of synthesis of andrographolide derivatives is summarized.

Key words: derivative, andrographolide, synthesis