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1.
以三乙胺为缚酸剂,通过α-芳氧丙酸与α-溴代嚬哪酮反应,合成了19个α-芳氧丙酸-2-氧代-3,3-二甲基丁醇酯类新化合物,其结构均经IR、1H NMR及元素分析确证。用小杯法初步测试了化合物的除草活性,结果表明,在施药剂量为0.225g/m2时,部分化合物具有较好的除草活性,其中化合物Ⅲp、Ⅲq和Ⅲr对苋菜Amaranthus retroflexus、油菜Brassica campestris和苜蓿Medicagosaliva生长的抑制率大多达到100%。  相似文献   

2.
N-α-氨基膦酸二苯酯的合成与除草活性   总被引:2,自引:0,他引:2  
通过芳氧丙酸与α-氨基膦酸二苯酯的缩合反应合成了8个未见报道的目 标化合物,利用红外光谱、核磁共振、质谱及元素分析确定了目标化合物的结构,初步的生物活性测定结果表明,目标化合物具有较好的除草活性,如化合物 Vg ,在浓度为10 mg/L下对单、双子叶植物的抑制率接近于2,4-D。  相似文献   

3.
以4,6-二氯-5-硝基嘧啶为起始原料,经过还原胺化、取代、醚化等一系列反应,得到11个未见文献报道的嘌呤氧基苯氧丙酸酯类化合物1a~1k,其结构经1H NM R和M S确认。初步生物活性测定表明:在200 mg/L下,所有目标化合物均表现出一定的除草活性,其中化合物1f((R)-2-(4-((9-(4-氯苯)-8-(三氟甲基-9H-嘌呤-6-基)氧)苯氧)丙酸丁酯)和1h((R)-2-(4-((9-(4-氯苯)-8-(三氟甲基-9H-嘌呤-6-基)氧)苯氧)丙酸乙酯)对靶标的抑制率几乎都达到100%。  相似文献   

4.
芳氧苯氧基丙酸酯类除草剂的应用进展   总被引:2,自引:0,他引:2  
芳氧苯氧基丙酸酯(简称APP)类除草剂是近二十年发展起来的活性很好的新型除草剂,用于防除一年或多年生禾本科杂草。本文主要综述了APP的发展历史、作用机理、主要品种以及应用研究进展。  相似文献   

5.
在温室盆栽条件下,测定了氟唑磺隆和氯氟吡氧乙酸异辛酯混用后对小麦田四种杂草的活性,同时采用Gowing法评价二者混用后的联合作用类型。结果表明,氟唑磺隆与氯氟吡氧乙酸异辛酯混用后对供试杂草的除草活性比单剂有所提高,但不同组合之间的除草活性差异不显著。混用后对供试杂草没有产生拮抗作用,大多数组合为相加作用,部分组合对禾本科杂草野燕麦和一年生早熟禾具有增效作用。综合考虑除草活性和经济成本,推荐氟唑磺隆和氯氟吡氧乙酸异辛酯的最佳配比范围为(3.75~30)+240(g a.i./hm~2),即有效成分比例为1∶(8~64)。  相似文献   

6.
通过芳氧乙(丙)酸与O,O'-二烃基硫代磷酰肼的缩合反应合成了8个未见报道的标题化合物,利用红外光谱、核磁共振、质谱和元素分析确定了化合物的结构。生物活性测试结果表明:目标化合物具有很好的选择性除草活性,其中化合物 3a、3b、3g和3h 对单子叶植物稗草和双子叶植物油菜均有较好的抑制作用,特别是对油菜的抑制作用尤为明显,其效果接近、有些甚至优于对照化合物2,4-D。  相似文献   

7.
通过取代苯氧异丁酸与12-(羟基亚氨基)十五内酯的反应,合成了取代苯氧异丁酰氧亚氨基十五内酯,并测定了其对苋菜的除草活性。所有化合物均经过1H NMR、13C NMR和元素分析确证。初步的生物活性测定结果表明,目标化合物 Ⅲa~Ⅲd 的EC50值分别为34.570、46.492、55.385、50.114 mg/L,其活性比对照药剂2,4-D(117.325 mg/L)高,而比苯磺隆(22.381 mg/L)低。  相似文献   

8.
(E)-O-芳酰基-α-氧代环十二酮肟的合成及除草活性   总被引:2,自引:0,他引:2  
以环十二酮为原料 ,制得中间体 (E) -α-氧代环十二酮肟 (Ⅳ)后 ,经酰化合成了九个 (E) - O-芳酰基 -α-氧代环十二酮肟 (Ⅴ) ,它们的结构得到元素分析、IR和 1HNMR的确证。生测结果表明 ,部分化合物具有良好的除草活性。对活性较高的 3还通过精密毒力测定 ,求得 IC50 值。中间体 在贝克曼反应条件下发生断裂反应生成 11-氰基十一酸 (Ⅶ) ,证实了 具有 (E) -构型的结构特征。  相似文献   

9.
为了研究2-仲丁氨基-5-(2-氯吡啶-4-基)-1,3,4-噻二唑(BCPT)的结构-活性关系和开发活性更高的新型除草剂,以BCPT为先导化合物,依据活性亚结构连接法,在吡啶环2-位上引入二芳醚类除草剂的典型结构单元——芳醚,设计并合成了一系列新的芳氧吡啶噻二唑类化合物,其结构经元素分析和1H NMR确证。初步除草活性测定结果表明,在500 mg/L剂量下,所有化合物的除草活性(抑制率0~45%)远低于先导化合物(抑制率72%~87%),说明吡啶环2-位上的氯原子可能对维持该类化合物的除草活性是必需的。  相似文献   

10.
为了寻找新的高生物活性农药,通过2-氨基-5-(1-邻氯苯氧乙基)-1,3,4-噻二唑与芳氧乙酰基异硫氰酸酯反应,合成了9个新的芳氧乙酰基硫脲,初步的生物活性测定结果表明,部分目标化合物具有良好的植物生长调节活性,其中2c、2d具有较好的生长素活性,其生长促进率分别为26.9%和27.2%.  相似文献   

11.
BACKGROUND: 4‐(3‐Trifluoromethylphenyl)pyridazine represents a new series of compounds with bleaching and herbicidal activities. RESULTS: A total of 43 novel 3‐(substituted benzyloxy or phenoxy)‐6‐methyl‐4‐(3‐trifluoromethylphenyl)pyridazine derivatives were synthesised, and their bleaching and herbicidal activities were evaluated through Spirodela polyrrhiza and greenhouse tests. Some compounds exhibited excellent herbicidal activities, even at a dose of 7.5 g ha?1. CONCLUSION: The results showed that a substituted phenoxy group at the 3‐position of the pyridazine ring and the electron‐withdrawing group at the para ‐position on the benzene ring were essential for high herbicidal activity. Copyright © 2011 Society of Chemical Industry  相似文献   

12.
Twelve 4-(substituted phenoxy)methyl-6-methyl coumarins were synthesised by the condensation of 4-chloromethyl-6-methyl coumarin with various phenols in the presence of potassium carbonate in dry acetone. The compounds were tested for their toxicity towards the mycelial growth of seven plant pathogenic fungi. Among the tested fungi, Pythium aphanidermatum, Colletotrichum falcatum, Drechslera oryzae, Alternaria alternata and Fusarium solani exhibited maximum sensitivity whereas Macrophomina phaseolina and Rhizoctonia solani were least sensitive to the test compounds. The 4-(4-tert-butylphenoxy)methyl and 4-(4-nitrophenoxy)methyl analogues possessed greatest toxicity towards the majority of the tested fungi.  相似文献   

13.
The crystal structures of a number of fungicidal azolylmethanes are compared. In the benzyl compounds [1-aryl-4,4-dimethyl-2-(1,2,4-triazol-1-yl)pentan-3-ones, the corresponding pentan-3-ols, and 1-(4-chlorophenyl)-3-(2-fluorophenyl)-2-(1,2,4-triazol-1-yl)propan-1-one], the benzyl and tert-butyl groups (or 4-chlorophenyl group) are trans, whereas in the analogous phenoxy compounds [1-(4-chlorophenoxy)-3,3-dimethyl-1-(1,2,4-triazol-1-yl)butan-2-one and the corresponding butan-2-ol], the tert-butyl groups are trans to the triazole and gauche to the phenoxy group. Coupling constants, determined by nuclear magnetic resonance (n.m.r.) spectroscopy, suggest that for some compounds there is one dominant solution conformation. Intramolecular hydrogen bonding, observed by infrared spectroscopy in two of the compounds, supports the findings by n.m.r. For some compounds, the crystal and solution conformations appear to be very similar, whereas in others they are quite different. Published data on the relative activity of the enantiomers of the benzyl- and phenoxy-compounds are discussed, but differences in the relative activity of enantiomers in the two series cannot be readily rationalised. It is concluded that different enantiomers may have different modes of binding at the active site.  相似文献   

14.
建立了一种简易而实用的残留分析方法 ,用于检测土壤与水中氰氟草酯及其 3种代谢产物 ,即(R)-2-[4-(4-氰基-2-氟苯氧基)苯氧基]-丙酸(ACID)、 (R)-2-[4-(4-氨基甲酰基-2-氟苯氧基)苯氧基]-丙酸(AMIDE)、(R)-2-[4-(4-羧基-2-氟苯氧基)苯氧基]-丙酸 (DIACID)。该方法仅用高效液相色谱法的梯度洗脱程序即可将 4种化合物有效分离 ,省去了需将氰氟草酯 (母体)衍生化反应再用气相色谱法检测这一复杂步骤。同时 ,该方法的添加回收率高。较低的 p H值对提高 4种化合物的提取效率很重要。  相似文献   

15.
Synthesis of new moth-proofing agents is necessary to overcome the damage caused by clothes moths and carpet beetles to hosiery and upholstery. In the present paper substituted benzyl 2-methyl-2-phenylpropyl ethers were synthesised and evaluated for moth-proofing activity. Two compounds were found to provide protection against larvae of Anthrenus fasciatus at levels of 1.0 and 10 g kg−1 respectively. The introduction of a methyl group in the para position of the benzene ring attached to C2 of the 2-methylpropyl chain (ring A) increased moth-proofing activity. The introduction of a phenoxy ring at the meta position of the benzyl nucleus (ring B) also increased activity, while the presence of a nitro group on the benzyl nucleus (ring B) decreased activity. © 1999 Society of Chemical Industry  相似文献   

16.
A new series of 5-(substituted phenoxy)pentyl 3-pyridyl ethers induced precocious metamorphosis in larvae of the silkworm, Bombyx mori. Both 2- and 4-pyridyl ethers were inactive, indicating that the 3-pyridine moiety was essential for the activity. Octyl, dodecyl and farnesyl 3-pyridyl ethers had no activity. Among the compounds tested so far, 5-(4-propylphenoxy)pentyl 3-pyridyl ether showed the highest activity. The activity fell off with increasing or decreasing length of the carbon chain between two oxygen atoms. Introduction of a methyl group at the 6 position of the pyridine ring completely eliminated the activity. Precocious metamorphosis induced by 3-pyridyl ethers was fully reversible by a simultaneous application of a small amount of tebufenozide, an ecdysteroid agonist, or methoprene, a JH agonist. © 1998 SCI.  相似文献   

17.
2-甲硫基-1-苯基乙酮苯甲酰腙类化合物的合成和生物活性   总被引:11,自引:3,他引:11  
为寻找新型结构的农药先导化合物,采用2-甲硫基-1-取代苯基乙酮与取代苯甲酰肼反应合成了11个2-甲硫基-1-苯基乙酮苯甲酰腙类化合物,其化学结构经质谱、1H核磁共振与元素分析确证。生物活性试验结果表明,部分化合物具有杀菌或杀虫活性,如2-甲硫基-1-(4-甲基苯基)乙酮-4-氯苯甲酰腙( Ⅲj )在500 mg/L时对黄瓜灰霉病菌B.cinerea、小麦赤霉病菌G.zeae具有良好的杀菌活性,其抑制率达到95%以上。  相似文献   

18.
取代吡唑并[4,5-e][1,3]噻嗪衍生物的合成及生物活性   总被引:5,自引:0,他引:5  
取代吡唑酰基异硫氰酸酯与杂环胺、磺酰胺反应 ,得到了加成产物取代吡唑酰基硫脲或关环产物吡唑并 [4 ,5- e][1,3]噻嗪。取代吡唑酰基硫脲化合物在三乙胺作用下也关环成吡唑并 [4 ,5- e][1,3]噻嗪。化合物结构均经 1HNMR、IR及元素分析确证 ,并对此加成、环化反应结果和机理进行了讨论。初步生物活性测试表明 ,这些化合物具有一定的杀菌、除草和植物生长调节作用。  相似文献   

19.
以3-氨基-2-氯吡啶(1)为起始原料,经重氮化、叠氮化、环合和酰氯化反应,生成1-(2-氯吡啶-3-基)-5-甲基-1H-1,2,3-三唑-4-甲酰氯(5),(5)与取代苯胺反应,制得13个未见文献报道的吡啶联三唑类化合物,其结构通过 1H NMR和LC-MS表征。初步生物活性测定结果表明:在500 mg/L质量浓度下,所有目标化合物对粘虫 Mythimna separate 均有一定的杀虫活性,部分化合物致死率达100%;但在100 mg/L下,除化合物ZJ-7的致死率仍达100%外,其余化合物的活性明显降低,甚至无活性。  相似文献   

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