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苯氧乙酰基噁唑烷类化合物的一锅法合成及生物活性
One-pot Synthesis,Crystal structure,and Bioactivity of N-Phenoxyacetyl-2,4,5-trisubstituted-1,3-oxazolidines
【作者】 付颖; 陈文更; 侯玉文; 王滨; 赵李霞; 叶非;
【Author】 Ying Fu;Wen-Geng Chen;Yu-Wen Hou;Bin Wang;Li-Xia Zhao;Fei Ye;Department of Applied Chemistry,Northeast Agricultural University;
【机构】 东北农业大学应用化学系;
【摘要】 [目的]为了进一步发现更广谱的安全剂,本文设计了一系列苯氧乙酰基噁唑烷衍生物,并进行了生物活性研究。[方法]苯氧乙酰基噁唑烷类化合物是通过邻氨基醇与醛或酮脱水环合成1,3-噁唑烷,进而与苯氧乙酰氯发生酰基化反应得到标题化合物。本文合成的合物经IR,1H NMR,13C NMR,ESI-MS和元素分析等手段进行结构表征。其中化合物4a还通过单晶进行结构表征。[结果]初步生物活性测试表明,合成的所有化合物能在一定程度上保护大豆免受苯氧乙酸类除草剂2,4-D丁酯的药害。
【Abstract】 In order to find a new safener,a series of N-phenoxyacetyl-l,3-oxazolidine were designed for test.N-phenoxyacetyl-l,3-oxazolidine derivatives were synthesized by the cyclization and acylation with P-amino alcohol,ketone and phenoxyacetyl chloride as the starting materials.All compounds were characterized by IR,1H NMR,13C NMR,ESI-MS and elemental analysis.The configuration of 4a was determined by X-ray crystallography.The preliminary biological tests showed that all products could protect soybean against injury caused by 2,4-D butylate to some extent.
【Key words】 Oxazolidine; synthesis; phenoxyacetyl; structural characterization; bioassay activity test;
- 【会议录名称】 中国化工学会农药专业委员会第十七届年会论文集
- 【会议名称】中国化工学会农药专业委员会第十七届年会
- 【会议时间】2016-07-28
- 【会议地点】中国河南郑州
- 【分类号】TQ450.1
- 【主办单位】中国化工学会农药专业委员会