Design, Synthesis And Biological Activity Study Of Caffeoylquinic Acid Derivatives

Natural products (NP) have traditionally played an important role in drug discovery and were the basis of early medicines. Over the last 15 to 20 years advances in X-ray crystallography and NMR, and alternative drug discovery methods such as rational drug design and combinatorial chemistry have placed great press upon NP drug discovery programmes. However, despite the promise of these alternative drug discovery methods, there is still a shortage of lead compounds progressing into clinical trials. This is especially the case in therapeutic areas where natural products have still played a central role in lead discovery. It is impossible to provide the diversity of compounds as natural products only by organic syntheses. Caffeoylquinic acids are widespread types of natural products occurring in nature. In this thesis, the research was carried out on the derivitives of natural caffeoylquinic acids.Caffeoylquinic acids are kinds of natural products with many biological activities. The hot research pionts are still focused on their isolation and pharmacological activities. It has served as a lead compound for the synthesis of derivatives to optimize their activity. Five series of target derivatives were designed and altogether 58 intermediate and target moleculars were synthesized, 50 of all of the moleculars are new compounds, they have not been reported to this day. The synthetic method and isolation of this sort of compounds are still need further improvement.