Study On The Synthesis Of Complexes Of Fluorobicyclo - Pyridone With Palladium (Ⅱ) Complexes

Now, many synthetic drugs are fluoride drugs that are used widely in the clinical application and cause the attention of chemists. Pyridone scaffolds are existed in a large number of natural products and biologically active molecules. Bicyclic pyridones possess a broad range of biological activities, including anti-tumor, anti-inflammatory and other biological activities. Thus the synthesis and research of fluorinated bicyclic pyridones compounds is great significance.Palladium (Ⅱ) complexes can improve the shortcomings of the platinum anticancer drugs, becoming a instead of platinum (Ⅱ) anticancer drug choice of priority. So far, a lot of palladium (Ⅱ) complexes has entered the stage of clinical trials, and been the research focus of anticancer drugs in the future. In the paper, the main work is as follows:The research progress of fluoride drugs, bicyclic pyridone compounds, palladium (Ⅱ) complexes and heterocyclic ketene aminalsare reviewed simply in the first chapter.In chapter two, an "one-step" synthesis method was developed by heterocyclic ketene aminals4react with methyl trifluoroacrylate5through alkali(K2CO3or Cs2CO3) as catalyst and reflux in1,4-dioxane. With this method, a series of new fluorinated bicyclic pyridone compounds6was synthesized; the yield is70%-93%.The third chapter we established a "three components and a pot" reaction method to synthesize novel palladium (Ⅱ) complexes. Using heterocyclic ketene aminals4, indolinedione compounds7and tetrakis (triphenylphosphine) palladium8as starting materials, a series of palladium (Ⅱ) complexes9was constructed succinctly and efficiently, the yield is65%-93%. All the structures of the compounds were confirmed by1HNMR,13CNMR, IR and HRMS spectroscopy. Among them, one of the compounds was confirmed through the X-Ray analysis.