【摘要】 为了合成新结构类型查尔酮衍生物,发现具有抗氧化活性的查尔酮类化合物,设计合成了查尔酮A和螺杂环B两种类型,共21个查尔酮类似物,结构经ESI-MS,ESI-HRMS和1H NMR确认.培养出螺杂环B1的单晶,通过X衍射确证了其为单斜晶系.其中螺杂环B为新结构类型化合物,通过1,3-偶极环加成反应,用不需加催化剂的"一锅煮"方法合成,该反应具有很好的立体选择性和区域选择性、且环境友好.用DPPH法测试了所有化合物的抗氧化活性,筛选出了多个对1,1-二苯基-2-三硝基苯肼(DPPH)自由基具有良好清除率的化合物,a环3,4-OH取代的两类化合物都具有良好的抗氧化活性,苯环邻位二羟基取代的查尔酮类化合物可能具有很好的抗氧化活性.更多还原

【Abstract】 To synthesize new structure type chalcone analogues,and obtain chalcone analogues with good antioxidant activity.Two types of chalcone analogs,chalcones A and spiro-heterocyclic B were designed and synthesized,and the structures of 21 compounds were characterized by 1H NMR,ESI-MS and ESI-HRMS.Single-crystal of spiro-heterocyclic B was cultured,and its single-crystal structure was determined by X-ray diffraction study.The crystal structure of B1 was monoclinic system,space group C2/c,with cell dimensions of a=21.350(3),b=8.6256(10),c=26.161(3).Spiro-heterocyclic B is the new structure type,and obtained by one-pot synthesis which is 1,3-dipolar cycloaddition reaction and no catalyst.The synthesis of spiro-heterocyclic B is not only high regioselectivity and stereoselectivity,but also environmentally friendly.The antioxidant activities in vitro were evaluated by 1,1-diphenyl-2-picrylhydrazyl(DPPH) assay.Many compounds,which can have strong activity of scavenging DPPH free radicals,were screened.In the 2 types of chalcones analogs,the compounds with 3,4-(OH)2 in "a" ring have excellent antioxidant activities.The chalcone analogs with o-dihydroxy in benzene ring maybe have good antioxidant activities.更多还原