Natural Product Indirubin And Isophthalic Three Phenolic Derivatives

Natural products play a very important role in chemistry, especially in organic chemistry because of their unique complexity of the chemical structure and their diversity of biological activity. They are always the major source of drugs and lead compounds. Extraction and isolation is a commonly used method, but often costs a lot. If we can find a suitable synthetic route, it will be possible to reduce costs and promote the development of drugs. In this dissertation, we have made a research on the synthesis of indirubin and phloroglucinol derivatives.Indirubin was a new drug with new structure that found by medical scientists in China in the mid-70s of the 20th century. It is an active ingredient of the traditional Chinese medicine Folium Isatidis with biological activities, such as antibacterial, anti-inflammatory, anti-tumor and enhancing the immune function and so forth. The compound has been applied to the treatment of patients with chronic myeloid leukemia. It has reliable clinical effects, less toxic side-effects. What's more, it shows no significant inhibition on the growth of bones. In the second chapter of this dissertation, we have summarized and optimized the synthetic route of indirubin and newly designed analog oxo-indirubin.The problem of antimicrobial resistance of pathogens is one of the outstanding characteristics of the current infectious diseases. In recent years, methicillin-resistant Staphylococcus aureus (MRSA) infections is infected easier than before, and the problem of drug resistance is more serious, which make the clinical treatment very difficult. Natural phloroglucinol derivatives has been widespread concerned because of its excellent antibacterial activity. In the third chapter of this dissertation, we made a retro-synthetic analysis of the two phloroglucinol derivatives which extracted from the Hypericum beanii in 2006. The four total synthetic routes have designed and experimental researches were explored.