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杀菌剂烯唑醇聚合物的合成及其生物活性 总被引:1,自引:0,他引:1
以杀菌剂烯唑醇1为底物与丙烯酰氯2反应合成了具有生物活性的可聚合单体(±)-(E)-1-(2,4-二氯苯基)-2-(1,2,4-三唑-1-基)-4,4-二甲基-1-戊烯-3-醇丙烯酸酯3,以IR,MASS和1H NMR对其化学结构进行了表征。该生物活性单体3与丙烯酸4共聚制得聚合物5。田间试验结果表明,以合成的杀菌聚合物5配成18%烯唑醇高分子缓释杀菌剂,对小麦纹枯病具有优异的防治效果,2、4、8 g a.i./100kg种子3个处理剂量,防效分别为56.82%、67.18%和81.00%,优于对照药剂12.5%烯唑醇WP的防治效果。 相似文献
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以2,4-二氯苯甲酸为起始原料,经酯化、肼解、成盐、闭环合成3-硫酮-4-氨基-5-(2,4-二氯)苯基-1,2,4-三唑(Ⅳ),然后与取代甲醛缩合生成中间体(Ⅴ),最后以乙腈为溶剂,K2CO3为催化剂,中间体Ⅴ与卤代烃于75℃反应2 h合成了8个含三唑Schiff碱硫醚衍生物(Ⅵa~Ⅵh),收率69%~78%,其结构经1HNMR、13CNMR、19FNMR、IR以及元素分析表征。初步生物活性测试结果表明,部分目标化合物对黄瓜霜霉病的抑制率达100%。 相似文献
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烯唑酮的光异构化反应的研究 总被引:1,自引:0,他引:1
烯唑酮,即1-(2,4-二氯苯基)-4,4-二甲基-2-(1,2,4-三唑-1-基)-1-戊烯-3-酮(Ⅰ)是近年来开发出来的高生物活性化合物。它可以直接被用作杀菌剂、植物生长调节剂和除草剂。然而该化合物更重要的应用是其反式异构体E-(Ⅰ)作为高效、广谱、内 相似文献
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2011年4月20日,山东省农药研究所完成的山东省科技攻关计划项目杀菌剂氟醚唑中间体‘苯唑醇'合成研究和新型杀虫剂SD-501中试通过了省科技厅的鉴定。山东省农药研究所自主设计了苯唑醇的合成工艺路线—由2,4-苯乙腈一锅合成2,4-苯乙酸乙酯、设计了合成2-(2,4-二氯苯基)-3-羟基丙酸乙酯的高效催化反应体系、设计了由2-(2,4-二氯苯基)-3-(1-氢-1,2,4-三唑-1-基)丙酸乙酯合成苯唑 相似文献
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高纯的Z—和E—二氯烯酮的获得方法 总被引:2,自引:0,他引:2
通过Knovenagel反应制备混合Z-和E-二氯烯酮、(Z+E)-1-(2,4-二氯苯基)-4,4-二甲基-2-(1,2,4-三唑-1-基)戊-1-烯-3-酮,该混合烯酮用乙醇处理得到纯度为99.97%的Z-烯酮,分离Z=烯酮后的混合烯酮经异构化反应得到纯度为99.73%的E-烯酮。 相似文献
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以 2 ,4 二氯苯乙酮为原料 ,经溴化得ω 溴 2 ,4 二氯苯乙酮 ,该化合物在以三乙胺做缚酸剂 ,温度 0℃的条件下与 1H 1,2 ,4 三氮唑反应 5h ,所得产物ω 1H 1,2 ,4 三氮唑基 2 ,4 二氯苯乙酮与盐酸羟胺在添加吡啶 ,加热回流条件下反应 4 5h ,得到的酮肟分别与乙酰氯、苯甲酰氯在以三乙胺做缚酸剂 ,常温条件下反应 12h ,合成了目标产物ω 1H 1,2 ,4 三氮唑基 2 ,4 二氯苯乙酮肟乙酸酯与ω 1H 1,2 ,4 三氮唑基 2 ,4 二氯苯乙酮肟苯甲酸酯两种肟羧酸酯 ,总收率分别为 32 4 %与 34 8%,化合物的结构经元素分析、气质联用及核磁共振所证实。对目标产物进行了初步的杀菌、杀虫与除草活性测定 ,结果表明 ,ω 1H 1,2 ,4 三氮唑基 2 ,4 二氯苯乙酮肟苯甲酸酯对粘虫 (Mythimnaseparata)具有杀虫活性。 相似文献
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Ludk Taimr 《大分子材料与工程》1994,217(1):119-128
A study has been carried out of the reaction of 6-ethoxy-2,2,4-trimethyl-1,2-dihydroquinoline (ethoxyquin, I ) with alkylperoxyls. In the presence of a relatively low concentration of 1-cyano-1-methylethylperoxyl, I reacts to form dimer IV (8-(6-ethoxy-2,2,4-trimethyl-1,2-dihydroquinolin-1-yl)-6-ethoxy-2,2,4-trimethyl-1,2-dihydroquinoline) as the main product and quinoline derivative III (2,4-dimethyl-6-ethoxyquinoline), as a side product, i.e., substances formed by the conversion of the aminyl II (6-ethoxy-2,2,4-trimethyl-1,2-dihydroquinolin-1-yl) alone. Smaller amounts of p-quinoneimine VI and o-quinoneimine VIII (2,2,4-trimethyl-2,6-dihydro-6-quinolone and 6-ethoxy-2,2,4-trimethyl-2,8-dihydro-8-quinolone) have been found; these substances are formed by further oxidation of II . In the presence of relatively high concentrations of tert-butylperoxyls, peroxide IX (6-tert-butylperoxy-6-ethoxy-2,2,4-trimethyl-2,6-dihydroquinoline) is formed as the main product. Substance IX thermally decomposes to form VIII , while in the presence of weak acids IX is converted into VI as the main product. Dimer IV is a medium-strength antioxidant which is gradually converted into 8-(6-ethoxy-2,2,4-trimethyl-1,2-dihydroquinolin-1-yl)-2,2,4-trimethyl-6-quinolone (XI) and 8-(6-ethoxy-3-hydroxy-2,2-dimethyl-4-methylene-1,2,3,4-tetrahydroquinolin-1-yl-)-2,2,4-trimethyl-2,6-dihydro-6-quinolone) (XII) . The methyl group in XI actively participates in the antioxidation process. When formed, nitroxide V (6-ethoxy-2,2,4-trimethyl-1,2-dihydroquinolin-N-oxyl) acts as an efficient antioxidant which, however, does not participate in the cyclic mechanism that is employed to explain the action of antioxidants of the HALS type. The antioxidant properties were evaluated on the basis of their effect on the course of the autoxidation of squalene. 相似文献
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Mahmoud A. Abbady Hussein S. El-Kahef Mohamed A. Abd-Alla Maymouna M. Kandeel 《Journal of chemical technology and biotechnology (Oxford, Oxfordshire : 1986)》1984,34(2):62-72
Cyclonucleophilic addition of N-phthaloylaminoacid chlorides (II on 4-(N-ary-lideneamino)-4′-nitrodiphenyl sulphides (I) in dioxane and triethylamine afforded 4-(4″-aryl-3″-phthalylamino-2″-oxo-azetidin-1″-yl)-4′-nitro-diphenyl sulphides (III). Hydrazinolysis of III yielded 4-(4″-aryl-3″-amino-2″-oxo-azetidin-1″-yl)-4′-nitro-diphenyl sulphide hydrochlorides (IV). Condensation of IV with anisaldehyde using ethanol and piperidine as a basic catalyst gave 4-(4″-aryl-3″-anisylidine amino-2″-oxoazetidin-1″-yl)-4′-nitrodiphenylsulphides (V) in good yields. Interaction of V with chloroacetyl chloride in dioxane and triethylamine produced 4-(4″-aryl-3″-substituted β-lactamyl-2″-oxo-azetidin-1″-yi)-4′-nitrodiphenyl sulphides VI. Oxidation of IV, V and VI using hydrogen peroxide/glacial acetic acid mixtures gave the corresponding sulphones (VII), (VIII) and (IX). Sulphones of the type IX were obtained by unequivocal synthesis through interaction of sulphone-anils VIII with chloroacetyl chloride. The antibacterial activities of some of these compounds were determined. 相似文献
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以间二氟苯为原料,经傅克酰化、水解、环合等反应制得三唑丁醇类抗真菌药物的重要中间体赤式-2-(2,4-二氟苯基)-3-甲基-2-[(1H-1,2,4-三唑-1-基)甲基]环氧乙烷,总收率44.6%,纯度98%以上(HPLC),工艺稳定,利于工业生产。 相似文献
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采用硅胶柱色谱、Sephadex LH-20凝胶柱色谱、开放ODS柱色谱以及HPLC等对海洋来源真菌Hypocreavirens的菌丝体进行化学成分分离,通过理化性质和波谱数据鉴定化合物的结构。从菌丝体的丙酮提取物中分离得到8个化合物,分别鉴定为1(10→6)Abeo-(22E,24R)-ergosta-5,7,9,22-tetraene-3α,11α-diol(Ⅰ)、24-甲烯基羊毛脂烷-8-烯-3β-醇(Ⅱ)、(22E,24R)-麦角甾-5,7,22-三烯-3β-醇(Ⅲ)、(22E,24R)-麦角甾-8,22-二烯-3β,5α,6β,7α-四醇(Ⅳ)、5α,9α-过氧-(22E,24R)-麦角甾-7,22-二烯-3β,6β-二醇(Ⅴ)、5α,8α-过氧-(22E,24R)-麦角甾-6,22-二烯-3β-醇(Ⅵ)、(22E,24R)-麦角甾-7,22-二烯-3β,5α,6β-三醇(Ⅶ)、3β,5α,9α-三羟基-(22E,24R)-麦角甾-7,22-二烯-6-酮(Ⅷ),其中化合物Ⅰ、Ⅱ、Ⅳ、Ⅴ、Ⅷ均为首次从该属真菌中分离得到,化合物Ⅲ、Ⅵ、Ⅶ为首次从该种真菌中分离得到。 相似文献
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The extraction of americium(III), curium(III), and lanthanides(III) from nitric acid by 2,6-bis-(5,6-dimethyl-[1,2,4]-triazin-3-yl)-pyridine and 2,6-bis-(5,6-dimethyl-[1,2,4]-triazin-3-yl)-4-methoxypyridine was studied. The physico-chemical properties of these ligands, such as the protonation and complexation constants, were also determined to describe the influence of different substituent groups. The selectivity of substituted-BTP was confirmed both in complexation and in solvent extraction experiments. The presence of an alkoxy-group in position 4 of the pyridine decreases the BTP selectivity. Influence of a long alkyl chain on protonation and complexation constants was also studied with 2,6-bis-(5,6-dimethyl-[1,2,4]-triazin-3-yl)-4-dodecyloxypyridine. 相似文献
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三唑类抗真菌药-氟康唑的研究进展 总被引:1,自引:0,他引:1
氟康唑是三唑类抗真菌药物,对于治疗深部真菌感染有显著疗效,毒副作用小,临床应用广泛。本文从氟康唑的抗真菌作用机制,药物动力学,临床应用范围,不良反应及氟康唑衍生物的合成等方面的研究进展进行了综述。 相似文献