3-芳基-1,3-苯并噁嗪的合成及其生物活性研究  

Studies on the Synthesis and Bioactivity of 3-Aryl-1,3-benzoxazines

作　　者：唐子龙[1,2] 崔美艳[1] 陈为文[1] 夏赞稳[1] 刘汉文[1,2] 

机构地区：[1]湖南科技大学化学化工学院,湖南湘潭411201 [2]理论化学与分子模拟省部共建教育部重点实验室,湖南湘潭411201

出　　处：《精细化工中间体》2011年第2期28-31,35,共5页Fine Chemical Intermediates

基　　金：国家自然科学基金资助项目(21042011);湖南省教育厅重点项目(10A034);湖南省博士后基金项目(2010RS4033)

摘　　要：以四氯化锡作催化剂,水杨醛、取代苯胺、硼氢化钠、多聚甲醛为原料合成了4种3-芳基-1,3-苯并噁嗪类化合物,收率为63%~73%（以氨甲基苯酚计,n/n）。产物化学结构经IR、1H NMR、13C NMR、MS和元素分析确证。测定了所合成化合物的杀虫和杀菌活性,结果表明合成化合物具有一定的杀菌活性,如5d在500 mg/L浓度下对稻纹枯病菌的防效为80%,5c在25 mg/L浓度下对油菜菌核病菌的抑制率为78.5%。Four 2-aryl-1,3-benzoxazines were prepared in 63%~73% yields from o-aminomethyl phenols and paraformaldehyde under catalysis of SnCl4.The structures of the target compounds were characterized with IR,1H NMR,13C NMR,MS and element analysis.The results showed that the catalytic activity of SnCl4 was higher than that of TsOH or H2SO4.The fungicidal activities of the title compounds were higher than their insecticidal activities.For instance,compound 5d showed 80.0% inhibitory rate against Rhizoctonia solani at the concentration of 500 mg/L,while compound 5c showed 78.65% inhibitory rate against Sclerotonia sclerotiorum at the concentration of 25 mg/L.

关 键 词：1 3-苯并噁嗪 合成 生物活性 

分 类 号：TQ316.341[化学工程—高聚物工业]