樟脑基苯甲酰胺类化合物的合成及生物活性研究

以天然樟脑为原料,经中间体樟脑肟和樟脑胺,以及樟脑胺与取代苯甲酰氯的N-酰化反应,合成得到9个樟脑基苯甲酰胺类化合物(3a～3i)。初步探索了合成条件,并通过FT IR、1H NMR、13C NMR、ESIMS和元素分析等多种手段对目标产物进行结构表征。生物活性测试表明,在50mg/L浓度下,所合成的化合物对5种植物病原菌均有一定的抑制作用,其中化合物3c(R=2-Cl)和3i(R=4-F)对苹果轮纹病菌的抑制率分别达97.5%和96.4%,化合物3i对小麦赤霉病菌的抑制率为95.7%。在100mg/L浓度下,化合物对油菜的胚根生长均显示良好的抑制活性,其中化合物3b(R=4-Cl)的抑制率达97.4%。     

樟脑基苯甲酰胺类化合物的合成及生物活性研究

以天然樟脑为原料,经中间体樟脑肟和樟脑胺,以及樟脑胺与取代苯甲酰氯的N-酰化反应,合成得到9个樟脑基苯甲酰胺类化合物(3a～3i)。初步探索了合成条件,并通过FT IR、1H NMR、13C NMR、ESIMS和元素分析等多种手段对目标产物进行结构表征。生物活性测试表明,在50mg/L浓度下,所合成的化合物对5种植物病原菌均有一定的抑制作用,其中化合物3c(R=2-Cl)和3i(R=4-F)对苹果轮纹病菌的抑制率分别达97.5%和96.4%,化合物3i对小麦赤霉病菌的抑制率为95.7%。在100mg/L浓度下,化合物对油菜的胚根生长均显示良好的抑制活性,其中化合物3b(R=4-Cl)的抑制率达97.4%。     

N-烃基-N''-取代苯基硫脲类化合物的合成

本文报道以丙酮为溶剂, 在三乙胺或三正丁胺的催化作用下, 通过异硫氰酸烃基酯与溴代邻氨基苯甲酸的加成反应合成了新的N-烃基-N'-取代苯基硫脲。     

樟脑基喹喔啉类化合物的合成及其生物活性

将D-(+)-樟脑用二氧化锡氧化制得樟脑醌,再与系列取代邻苯二胺化合物缩合,合成得到19个樟脑基喹喔啉类化合物(3a～3s),并用UV-Vis、 ¹H NMR、 ¹³C NMR、 FT-IR和HR-MS(ESI)进行结构表征。初步的抑菌和除草活性测试表明：在用药量为50 μg·mL^-1时,目标化合物对花生褐斑病菌、小麦赤霉病菌、黄瓜枯萎病菌、苹果轮纹病菌、番茄早疫病菌、玉米小斑病菌、西瓜炭疽病菌以及水稻纹枯病菌等8种植物病原菌具有一定的抑制活性,其中化合物樟脑基5,8-二溴喹喔啉3r(R¹=R⁴=Br,R²=R³=H)对苹果轮纹病菌的抑制率达78.6%,优于阳性对照百菌清。在用药量为100 μg·mL^-1时,化合物樟脑基6-氟喹喔啉3f(R³=F, R¹=R²=R⁴=H)和樟脑基7-氟喹喔啉3g(R²=F, R¹=R³=R⁴=H)对油菜胚根生长的抑制率分别为75.8%和68.5%,均优于阳性对照丙炔氟草胺。      

N-烃基-N′-取代苯基硫脲类化合物的合成

N-烃基-N′-取代苯基硫脲具有多种重要的生物活性,如抗结核、抗真菌、除草及促进植物生长等功效。为了进一步研究此类化合物的性质,以期得到有生物活性的化合物,我们以丙酮为溶剂,在三乙胺或三正丁     

取代苯基呋喃甲酸长链烷基酯的合成及生物活性

取代苯基呋喃甲酸长链烷基酯的合成及生物活性司宗兴＊孙亚秋汪海涛（中国农业大学应用化学系北京１０００９４）关键词苯基呋喃甲酸酯，合成，杀菌活性１９９６－０６－１７收稿，１９９６－１２－０５修回取代芳基呋喃甲酸是一类很好的活性基团，它的酯在医学上用做镇痛...     

O—烷基苯基硫代磷酰取代硫脲的合成（Ⅲ）：含P—C键化合物的…

利用Ｏ－烷基苯基硫代磷酸酸异硫氰基酯与胺与胺的加成反应，合成了两系列Ｏ－烷基苯基硫代磷酰取代硫脲化合物，经元素分析、ＩＲ和＾１ＨＮＭＲ确定了它们的结构，并进行了除草活性的测试。     

硫脲化合物的合成及其生物活性

硫脲化合物的合成及其生物活性董燕红，司宗兴（北京农业大学应用化学系北京１０００９４）关键词噻二陛－甲酰基，硫脲，胺类，合成，生物活性酰基硫脲在抗真菌、抗结核、抗病毒、除草以及调节植物生长方面具有广泛应用［１，２］。１，２，３－噻二唑杂环作为有效前体正...     

合成光学活性樟脑

目前按所谓“四步法”生产的合成樟脑是消旋的。天然樟脑是光学活性的,大多数为右旋体。左旋天然樟脑较为稀少。藤原羲人,松原羲治等曾报道合成光学活性樟脑,其中龙脑脱氢反应是在有机溶剂的存在下进行的,产物的光学纯度为原料的70%左右。     

Synthesis and biological activity of ethyl 2-(5-methyl-3-arylisoxazole-4-carboxamido)-4-alkylthiazole-5-carboxylate

A series of novel ethyl 2-(5-methyl-3-arylisoxazole-4-carboxamido)-4-alkylthiazole-5-carboxylates I-1-6 were synthesized. The structures of all target compounds were characterized by ¹H NMR, ¹³C NMR, IR, MS and elemental analyses. Their fungicidal and herbicidal activities were evaluated. The results of preliminary bioassays show that the title compounds I-4 possess 20–50% inhibition against most of the tested plants at the dosage of 150 g ai/ha, while the title compounds I-1-5 possess 32–58% inhibition against FusaHum graminearum, Thanatephorus cucumeris, Botrytis cinereapers and Fusarium oxysporum in vitro at the concentration of 100 mg/L.     

Synthesis and biological activity of novel N-(3-furan-2-yl-1-phenyl-1H-pyrazol-5-yl) amides derivatives

A series of novel N-(3-furan-2-yl-1-phenyl-1H-pyrazol-5-yl) amides derivatives were designed and synthesized. Their structures were confirmed by ¹H NMR, ¹³C NMR and HRMS. All title compounds were evaluated for their herbicidal and antifungal activities. Preliminary bioassay results indicated that the title compounds showed good to moderate herbicidal activity at 1000 mg/L. Compound 6q presented the best activity against Digitaria sanguinalis (L) Scop., Amaranthus retroflexus L. and Arabidopsis thaliana with an inhibition degree of five. Compound 6d also showed an inhibition degree of five against D. sanguinalis. In addition, at 50 mg/L, most compounds exhibited good in vitro antifungal activity against Sclerotinia sclerotiorum, with compound 6c showing over 90% antifungal activity against S. sclerotiorum and Pellicularia sasakii.     

2-甲基-6-硝基苯磺酰脲衍生物的合成及生物活性

设计合成了一系列2-甲基-6-硝基苯磺酰脲衍生物(4a~4p),通过核磁共振氢谱(1H NMR)和高分辨质谱(HRMS)对其结构进行了确认.盆栽法除草测试结果表明,在300 g/ha剂量下,目标化合物具有优异的芽前或芽后除草活性.进一步筛选发现,在75 g/ha剂量下,化合物4b,4g,4h,4l和4p对油菜、反枝苋和稗草具有98%以上的除草活性,与对照药单嘧磺隆(100%)和氯磺隆(≥96.3%)相当.另外,部分化合物对真菌也表现出一定的抑制效果,其中化合物4l对油菜菌核病菌的半最大效应浓度EC50=9.20 mg/L(对照药多菌灵的EC50=5.79 mg/L).     

取代苯基吡唑类化合物的合成及其除草活性

以1′-(4-氯-2-氟-5-甲基苯基)-4′,4′,4′-三氟-1,3-丁二酮为原料,合成了一系列具有取代苯基吡唑结构的新化合物.化合物结构经¹HNMR,IR,CIMS和元素分析确认.初步生物活性测试表明,所合成的化合物对阔叶杂草具有较高的活性.     

Synthesis and biological activity of novel 2-(3-trifluoromethylphenoxy)-4-trifluoromethylthiazole-5-carboxamide derivatives

Novel 2-(3-trifluoromethylphenoxy)-4-trifluoromethylthiazole-5-carboxamides were designed and synthesized utilizing ethyl 3-amino-4,4,4-trifluoro-2-butenoate as a starting material via six steps. Subsequently, their biological activities were evaluated in the greenhouse. Results indicated that several compounds have some insecticidal or fungicidal activity at 600 g ai/ha and 300 g ai/ha, respectively.     

Synthesis and bioactivity of novel (3-chloro-5-(trifluoromethyl)pyridin-2-yloxy)phenyl containing acrylate and acrylonitrile derivatives

Fifteen novel (3-chloro-5-(trifluoromethyl)pyridin-2-yloxy)phenyl containing Baylis-Hillman adduct derivatives were designed and synthesized. Evaluation of their biological activities showed that methyl 2-((3-(3-chloro-5-(trifluoromethyl)pyridin-2-yloxy)phenoxy)(phenyl)methyl)acrylate (2g) exhibited efficient broad-spectrum fungicidal activity, with 100% control of wheat powdery mildew and cucumber downy mildew and 98% control of cucumber anthracnose at 400 g ai/ha. Some of the other title compounds 2, 3 and two Baylis-Hillman bromide intermediates (11a, 11b) had moderate to good fungicidal activity.     

2-芳甲酰氨基硫羰基-3-异噻唑酮及4-氰基-5-甲硫基-2-芳甲酰氨基硫羰基-3-异噻唑酮的合成与生物活性

通过3-羟基异噻唑(4)和4-氰基-5-甲硫基-3-羟基异噻唑(5)分别与芳酰基异硫氰酸酯(3)反应,合成标题化合物2-芳甲酰氨基硫羰基-3-异噻唑酮(6a_6f)和4-氰基-5-甲硫基-2-芳甲酰氨基硫羰基-3-异噻唑酮(7a_7e),对此反应及产物的结构特点进行了探讨.     

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 Sulfonylureas Containing Thiadiazol Moiety

Thirteen novel sulfonylureas containing thiadiazole moiety were synthesized in a two-step reaction. Their structures were determined using IR, ^1H NMR, HRFTMS, and elemental analysis. Herbicidal activities of these compounds were determined in the green house bio-assay. The results show that four compounds among them exhibit some activity toward four tested herbs.