Synthesis Of Salvianolic Acid E Derivatives And Preparation Of Dibenzophenone Series Fluorinated Compounds

1.Water-soluble salvianolic acid is an important active component of Salvia milt-iorrhiza,which mainly includes salvianolic acid A,B,C,E,salvianolic acid,protocatechuic aldehyde and so on.These components have a wide range of pharmacological activities,esp-ecially in the treatment of cardiovascular and cerebrovascular diseases,and have protective effects on myocardial cells,liver and so on.They have been widely used in clinical practice.In this paper,based on the previous laboratory work,salvianolic acid derivatives(3-(3,4-dimethoxyphenyl)-2-hydroxypropionate)were synthesized,and then 3-(3,4-methoxyphe-nyl)-2-(2,3-dimethoxy-6-carboxylic acid vinyl phenyl)acrylic acid(I)was docked with cin-namyl alcohol,3,4-dimethoxyphenylethylamine and 3-butyne-1-ol to synthesize salvianol-ic acid E derivatives,respectively.The results are as follows: A new synthetic route of ethyl-3-(3,4-dimethoxyphenyl)-2-hydroxypropionate was designed.The process is simple and easy to operate.The yield of the product can be stabilized at 11%.Three derivatives of salvianolic acid E were synthesized.2.Fluorine is a very special element.In modern medicine and agricultural chemistry,some physiological activities of compounds can be changed and improved by introducing fluorine atoms.Carbonyl groups are also ubiquitous in many natural product molecules with strong biological activity.In this paper,we mainly studied the oxidation rearrangement reaction of alpha,alpha-diaryl allyl alcohol and perfluoroiodobutane to obtain alpha-aryl-beta-perfluoroalkylated benzophenones containing fluorine under the condition of only copper as catalyst and without any ligands.The results are as follows:In this part,the fluorinated benzophenones containing alpha-aryl-beta-perfluoroalkyl-ation were synthesized by using alpha,alpha-diaryl allyl alcohol as substrate,perfluoroi-odobutane as reaction reagent,cupric acetate as catalyst,cesium carbonate as base,dioxane as reaction solvent at 100 ～C for 24 hours.The yield of fluorinated benzophenones was as high as 85%.The novelty of this subject was that the reaction system did not need ligands and had manipulation.It has the characteristics of simple,high efficiency and high utilization rate of atoms.According to the reaction results,the reaction mechanism was inferred.