橙酮衍生物的合成、晶体结构及除草活性

设计合成了17个橙酮类化合物, X射线单晶衍射分析显示其双键为Z型. 测定了它们对稗草地上部分和油菜根长的抑制率. 结果表明, 部分化合物对双子叶植物油菜有较好的活性, 表现出良好的选择性. 当浓度为100 μg/mL时, 化合物15对油菜胚根的抑制率达到88.5%,接近商品除草剂甲基磺草酮的活性, 当浓度为10 μg/mL时其对油菜胚根的抑制率达到81.3%. 初步构效关系研究表明, 橙酮A环上的电子效应以及分子的亲水与疏水性对保持其活性有重要的作用,为进一步结构优化提供了依据.     

4-吡唑基-2-芳氧基嘧啶类化合物的合成及除草活性

以2,4-二氯嘧啶为起始原料, 利用两个氯原子的活性差异, 经4-吡唑基-2-氯嘧啶合成了一系列4-吡唑基-2-芳氧基嘧啶类化合物, 通过¹H NMR和元素分析对所合成的化合物进行了结构表征. 初步生物活性测定结果表明, 所合成的化合物都表现出一定的除草活性. 当嘧啶环2位的氯原子被芳氧基取代后, 化合物的除草活性均有不同程度的提高, 例如5c和4a相比, 100 μg•mL^－1时化合物对油菜的抑制率由15.7%提高到85.4%, 对稗草的抑制率由原来的11.6%提高到84.0%.     

新磺酰脲类化合物的合成及除草活性

新磺酰脲类化合物的合成及除草活性;嘧啶;合成;除草剂     

新型香豆素衍生物的设计、合成及除草活性研究

以(未)取代的间苯二酚与β-酮酸酯类化合物为起始原料,在酸的催化下发生Pechmann 反应,合成了4个关键中间体--7-羟基香豆素衍生物(1a~1d),其与芳氧乙(丙)酰氯作用,合成了8个结构新颖的7-芳氧乙酰氧基香豆素衍生物(2a~2h),其结构经¹H NMR、¹³C NMR和元素分析表征。油菜平皿法和稗草小杯法的测试结果表明,目标化合物对双子叶植物油菜根长的抑制效果好,与阳性对照药2,4-D相当,并表现出一定的构效关系。进一步的温室盆栽实验(50 g/亩)表明,茎叶处理时,部分目标化合物(如2a~2e)对双子叶植物的抑制率为100%,与2,4-D的防效相当,具有作为先导化合物进一步优化的价值。      

Synthesis of Functionalized Dihydrofurocoumarin Derivatives from 3-Aminoalkyl-4-hydroxycoumarin

Some dihydrofuro-fused coumarin derivatives were synthesized from 3-aminoalkyl-4-hydroxycoumarin via in situ generation of N-ylide. The 3-aminoalkylated 4-hydroxycoumarin derivatives were synthesized from one-pot, three-component reaction of 4-hydroxycoumarin, aryl aldehydes, and secondary amines in ethanol at room temperature. Again, when salicylaldehyde was employed instead of benzaldehyde, interestingly pyranocoumarins were obtained. The reaction protocol can be further explored toward the synthesis of many other heterocyclic fused dihydrofurans.     

苯环2-位不同酯基取代的磺酰脲类化合物的合成及其除草活性

以正在开发的磺酰脲类超高效除草剂NK94827[N'-(4'-甲基嘧啶-2'-基)-2-甲氧羰基苯磺酰脲]的基本结构为基础,设计合成了18个苯环2位不同酯基取代的的新型磺酰脲类化合物,产物结构均经¹HNMR及元素分析确证.经油菜平皿法和盆栽试验测试除草活性,所合成的部分磺酰脲化合物的除草活性高.     

Synthesis and Herbicidal Activity of Novel Sulfonylurea Derivatives

Sulfonylurea herbicides have been applied worldwide in agriculture. Some sulfonylurea residues might exist in soil longer than that people expected. However, flupyrsulfuron-methyl-sodium which was firstly reported as a new 5-substituted sulfonylurea herbicide has less than one month residual life. Therefore, 5-substituted benzenesulfonylureas are potential molecules to regulate its residual situation. In order to develop new sulfonylurea derivatives, the substituent on the critical 5-posotion of the benzene...     

新磺酰脲类化合物的合成及生物活性

以正在开发的新磷磺酰脲除草剂N-[2′-(4′-甲基)嘧啶基]-2-硝基苯磺酰脲的研究为基础,设计合成了19个脲桥经修饰的磺酰脲类化合物以及3个新型嘧啶中间体,产物结构经¹HNMR谱及元素分析确证.盆栽试验和离休ALS酶研究结果表明,所合成的化合物均表现出一定的除草活性,部分化合物的除草活性较好.     

Synthesis and Herbicidal Activity of Novel Phenoxysulfonylureas Derivatives

Thirteen novel phenoxysulfonylureas derivatives were synthesized, and their structures were confirmed by MS, NMR and element analysis. The herbicidal activity and structure-activity relationship were also investigated. The results of preliminary active tests indicate that the compounds show moderate herbicidal activity.     

Synthesis,Crystal Structure and Herbicidal Activity of N-（4-Methylbenzyl）-4-（3-fluorophenyl）-4-piperidinol Hydrochloride

A novel compound N-（4-methylbenzyl）-4-（3-fluorophenyl）-4-piperidinol hydrochloride has been synthesized and its structure （C19H23ClFNO, Mr = 335.83） was characterized by elemental analysis, IR, ^1H NMR, MS and single-crystal X-ray diffraction analyses. The crystal belongs to the triclinic system, space group P1 with a = 7.2163（6）, b = 10.7905（9）, c = 12.2651（10） A, α = 109.576（2）,β = 98.407（2）,γ= 95.956（2）°, V= 878.14（13）A3, Z = 2, Dc = 1.270 g/cm^3,μ = 0.231 mm^-1, F（000） = 356, S = 1.100, the final R = 0.0525 and wR = 0.1425 for 3206 unique reflections （Rint = 0.0140） with 2736 observed ones （I 〉 2σ（I））. The piperidine ring exhibits a chair conformation. The dihedral angle made by the methyl- and fluoro-substituted benzene rings is 66.84（7）°. There are some intra- and intermolecular hydrogen bonding interactions among the molecules, which stabilize the whole crystal structure. The preliminary biological activity tests indicate good herbicidal activity for the title compound, in particular against the roots of some tested plants （such as Brassica campestris L. and Echinochloa crusgallis L.）.