The Synthesis Of Gem-difluorinated 1,1-diarylethylene Compounds And Their Bioactivities Evaluation

Fluorine atoms with high ionization potential and higher electronegativity,fluorine polarization rate is low,the atomic radius is lesser,introducing fluorine atoms into organic molecules usually has a great influence on its properties.Due to this important feature,fluorine containing organic compounds have been widely used in various pharmaceutical and material fields.The physical chemistry and biological properties of the molecules can be improved by the introduction of the difluoroalkyl group to the molecule.As a result,the high-efficiency synthesis of difluoroalkyl compounds has attracted more and more attention.In this paper,we studied the palladium catalyzed by alpha and alpha and alpha iodine fluorinated phenyl ethyl ketone compounds with alkynes and aryl boric acid reaction of three component,with 1-benzene in high yield of 2,2-methyl-formyl two fluorine diphenyl ethylene,and have excellent stereoselectivityThe first part introduced the synthesis of 1,1-2 aryl ethylene compounds by the three components of?,?,?--iodifluorophenone,alkynes and aryl boric acid.Firstly,the reaction conditions such as catalyst,solvent,alkali and temperature were screened and the optimum reaction conditions were obtained.Specifically,under the protection of nitrogen,5 mol%Pd?PPh₃?₄ as catalyst,potassium phosphate?2 equivalent?as alkali,toluene as solvent,and 6to 12 hours under 60?conditions.A novel 1-benzoyl difluoromethyl-2,2-diphenyl ethylene compound was synthesized by the reaction of the three components,and all the compounds were confirmed by nuclear magnetic and mass spectrometry.At the same time,the reaction mechanism of the reaction was studied.In addition to 1-benzene formyl fluorine 2,2-methyl-2 diphenyl ethylene compounds for the structure of the substrate in a series of translational research,get different fluoride group instead of 1,1-2 aryl vinyl compounds.In the second part,the bioactivity of 1,1-diaryl ethylene compounds was studied.The biological activity of target product was simulated by computer aided method.After that,the antitumor activity was tested in vitro.Through the use of Combretastatin A-4?CA-4?as the positive control,in six kinds of human tumor cells called HeLa,A549,HTC-116 and HepG2,MKN45 and MGC-803 test on the selected compound antitumor activity,indicating A benzoyl 2 fluorine-1,1-2 skeleton aryl vinyl compounds have certain antiproliferative activity of human tumor cells,can pass the structure-activity relationship of further research and development of potential new antitumor drugs.