水杨醛席夫碱功能化荧光素化合物的合成

以对氨基苯甲酸甲酯和水合肼为原料,经酰胺化反应制得对氨基苯甲酸甲酰胺与水杨醛还原氨化反应生成水杨醛类席夫碱1,化合物1在丙酮溶剂中与三聚氯氰亲核取代得到一缩产物对氨基苯甲酰水杨醛肼腙三嗪产物2,然后以荧光素和水合肼的合成产物荧光素酰肼3与化合物2在四氢呋喃溶液中45~50℃反应得到目标产物二缩产物荧光素酰肼三嗪水杨醛席夫碱4,并通过IR与~1H NMR对其结构进行表征。     

L-(-)-二邻甲基苯甲酰酒石酸的合成研究

以邻甲基苯甲酸和二氯亚砜为原料,合成了邻甲基苯甲酰氯;再以L-酒石酸与邻甲基苯甲酰氯反应,生成L-(-)-二邻甲基苯甲酰酒石酸酐;该酸酐经水解得到目标化合物L-(-)-二邻甲基苯甲酰酒石酸。探讨了邻甲基苯甲酰氯用量、回流反应时间和酸酐水解时间等对合成反应的影响。结果表明,在L-酒石酸与邻甲基苯甲酰氯的摩尔比为1.0∶2.4、回流反应时间为3h、酸酐水解时间为2h的最佳工艺条件下,总产率为88.2%。     

新型磺酰脲类化合物的设计、合成与除草活性

[目的]利用中间体衍生化方法,设计合成一系列氨基磺酰脲类新化合物。[方法]以(取代)邻氨基苯甲酸为起始原料,通过与固体光气合环得到靛红酸酐,再与胺开环得到邻氨基苯甲酰胺中间体,最后再与嘧啶磺酰氯缩合得到磺酰脲类化合物。[结果]目标化合物结构经核磁表征。[结论]生物活性测定结果表明该类化合物具有较好的除草活性,可有效防除马唐和苘麻。并初步探讨了其结构活性关系。     

缩氨基硫脲类受体的合成和表征

采用对甲基苯胺和高锰酸钾氧化生成对氨基苯甲酸,后者用磷酸三甲酯N甲基化,生成对二甲氨基苯甲酸,其经酯化、肼解得到对二甲氨基苯甲酰肼（A）。A与异硫氰酸对硝基苯酯反应,制得N-对二甲氨苯甲酰胺基-N’-对硝基苯基硫脲,收率76％;同理,对硝基苯肼与异硫氰酸对甲苯酯反应,得到N-对硝基苯胺基-N’-对甲苯基硫脲,收率41％。通过元素分析,IR,1HNMR对化合物的结构进行了表征。     

邻氨基苯甲酰甲基异(硫)脲类衍生物的合成与杀虫活性初步研究

以杀虫剂氯虫苯甲酰胺为先导,设计并合成了8个邻氨基苯甲酰甲基异(硫)脲类化合物。目标化合物的结构经核磁表征确认。初步生物活性测试结果表明,此类化合物对小菜蛾具有较好的杀虫活性。     

薄层色谱法跟踪N-萘乙酰基-N''''-邻甲氧基苯甲酰氨基硫脲的合成

通过α-萘乙酸和SOCl2在无水苯中反应制得α-萘乙酰氯,然后与硫氰酸钾反应生成α-萘乙酰基异硫氰酸酯,再与邻甲氧基苯甲酰肼进行加成反应,生成新型N,N'-萘乙酰基取代邻甲氧基苯甲酰氨基硫脲化合物,用薄层色谱法跟踪最后一步反应,确定了反应时间.产物经1H NMR、 IR和元素分析测定.生物活性试验结果表明对稻子根生长具有促进作用,对大肠杆菌和枯草杆菌无明显抑菌作用.     

α-(2,4-二氯-5-氟苯甲酰)-β-取代氨基丙烯酸酯的合成

以中间体2,4-二氯-5-氟苯甲酰乙酸甲酯为原料．通过与原甲酸三乙酯进行缩合,再与氨基化合物发生亲核取代反应,制备得到8种α-(2,4-二氯-5-氟苯甲酰)-β-取代氨基丙烯酸酯衍生物,并对它们的反应活性进行了研究。     

邻氟苯甲酰基硫脲化合物的合成研究

以邻氟苯甲酸为原料,经酰氯化、酰化生成邻氟幕甲酰基异硫氰酸酯后,与2-氨基嘧啶进行加成反应,合成了邻氟苯甲酰基硫脲化合物,产率为71.03%.探讨了影响反应的主要因素,并采用IR、IHNMR对产物进行了表征.     

磺酰脲化合物的合成及除草活性研究

合成了9种未见文献报导的磺酰脲化合物,其结构经元素分析、IR和1H NMR表征.生物活性研究表明：2 (4甲氨基6异丙氧基三嗪2基)氨基甲酰基氨基磺酰基 苯甲酸甲酯(Ⅲa)具有良好的除草活性.     

2-邻羟基苯基-5-芳基-1,3,4-(口恶)二唑化合物的合成

邻羟基苯甲酸甲酯与水合肼为原料制得邻羟基苯甲酰肼,再与芳酰氯反应,得到相应的N,N′-二酰基肼,后在POCl3作用下,脱水环化生成系列2-邻羟基苯基-5-芳基-1,3,4-(口恶)二唑化合物.通过元素分析,IR,1HNMR和MS对其结构进行了表征,并对其裂解途径进行了探讨.     

苯并噻二唑类和苯并噻唑类化合物的合成及生物活性

合成了33个苯并噻唑和苯并噻二唑类化合物，所有新化合物经过元素分析、^1H NMR和IR确认，初步的离体生物活性结果表明：I-09、II-01、II-05、II-06、III-01、III-03和III-05的活性较好，对黄瓜灰霉病菌具有良好的抑制作用。活体抗菌诱导生物活性测定结果表明：I-04、I-07、II-09、II-13、III-02、III-071000mg／L在离体条件下对黄瓜灰霉病没有抑制作用，在活体条件下有一定的抑制作用，抑制率在55．0％-84．4％，表明具有良好的诱导抗性活性。     

新型邻甲酰氨基苯甲酰胺类杀虫剂的研究进展

介绍了新型邻甲酰氨基苯甲酰胺类杀虫剂的研究进展。根据具体化学结构类型不同分为五大类，概述了具有较好生物活性的化合物，介绍了氯虫酰胺的创制经纬和合成方法。     

Synthesis, characterization and morphology of polyanthranilic acid micro- and nanostructures

Polyanthranilic acid (PANA) nanofibres, nanorods, nanospheres and microspheres were synthesized by polymerization of anthranilic acid using ammonium peroxydisulfate (APS) as oxidant without hard or soft templates. Polymerization of anthranilic acid was carried out in aqueous solutions of strong (hydrochloric) and weak (acetic) acids. The influence of synthetic parameters such as oxidant, initiator, dopant acid and its concentration, redox initiator, and reaction medium on the morphology and particle size of PANA have been investigated. PANA nanofibres and nanorods were obtained via redox polymerization of anthranilic acid initiated by FeSO₄ as redox initiator. PANA nanospheres and nanofibres were also obtained when used aromatic amines as initiators. When polymerization carried out in the solution of weak (acetic) acid the microsphere morphology obtained and the particle size increase with increasing the concentration of weak acid. PANA nanorods were obtained also by polymerization of anthranilic in ethanol-water mixture unlike interfacial polymerization of anthranilic acid (in chloroform-water) that give PANA microspheres. The morphology and particle size of PANA was studied by scanning electron microscope (SEM) and transmission electron microscope (TEM). The average diameter of nanostructures obtained ≤100 nm. The optical bandgap of microspheres and nanofibers polymeric products were determined using UV-vis spectroscopic technique and found to be 2.0 eV and 1.6 eV, respectively. The bandgap decreased with decreasing the particle size. IR spectrum confirmed the structure of PANA nanofibres (synthesized with FeSO₄ as redox initiator) in emeraldine form. The thermal stability of polymer obtained was determined by thermal gravimetric analysis (TGA). The molecular weight was determined also by gel permeation chromatography (GPC).     

Studies on cation-exchange resins: I. Chelating properties of cation exchangers prepared from cold extracted commercial cashewnutshell liquid

Four weakly acidic cation exchangers have been prepared, one by the polycondensation of cold extracted commercial cashewnutshell liquid (C-CNSL) with formaldehyde and the other three by the co-condensation of C-CNSL with formaldehyde and each of the compounds gallic acid, anthranilic acid and 2-mercapto-benzothiazole. The resins have been investigated for the selective uptake of cations from external solutions of different pH. The resin prepared by polycondensation of C-CNSL and the one prepared by its co-condensation with gallic acid showed comparatively specific absorption of Fe²⁺ ions.     

Selection of alcohols through Plackett-Burman design in lipase-catalyzed synthesis of anthranilic acid esters

Lipase-catalyzed synthesis of esters of anthranilic acid was attempted by employing alcohols of carbon chainlength C₁–C₁₈ using Plackett-Burman experimental design. Of the alcohols employed, methanol, decanol, cetyl alcohol, and stearyl alcohols showed 99.9% significance. Esterification of anthranilic acid with methanol gave the highest yield at 45.6%. This study allows the selection of better alcohols for esterification of anthranilic acid.     

双酰胺类化合物在新农药创制中的研究进展

综述了邻二甲酰胺类化合物和邻甲酰氨基苯甲酰胺类化合物,介绍了各自的代表物氟虫双酰胺和氯虫苯甲酰胺以及这两类化合物的类似物,并展望了双酰胺类化合物的研究趋势。     

Anthranilic acid assisted preparation of Fe3O4–poly(aniline‐co‐o‐anthranilic acid) nanoparticles

Magnetic Fe₃O₄–poly(aniline‐co‐o‐anthranilic acid) nanoparticles were prepared by a novel and simple method: anthranilic acid assisted polymerization. The synthetic strategy involved two steps. First, Fe₃O₄ nanoparticles capped by anthranilic acid were obtained by a chemical precipitation method, and then the aniline and oxidant were added to the modified Fe₃O₄ nanoparticles to prepare well‐dispersed Fe₃O₄–poly(aniline‐co‐o‐anthranilic acid) nanoparticles. Fe₃O₄–poly(aniline‐co‐o‐anthranilic acid) nanoparticles exhibited a superparamagnetic behavior (i.e., no hysteresis loop) and high‐saturated magnetization (M_s = 21.5 emu/g). The structure of the composite was characterized by Fourier‐transform infrared spectra, X‐ray powder diffraction patterns, and transmission electron microscopy, which proved that the Fe₃O₄–poly(aniline‐co‐o‐anthranilic acid) nanoparticles were about 20 nm. Moreover, the thermal properties of the composite were evaluated by thermogravimetric analysis, and it showed excellent thermal stability. © 2006 Wiley Periodicals, Inc. J Appl Polym Sci 102: 1666–1671, 2006     

Precursor-directed syntheses and biological evaluation of new elansolid derivatives

The antibiotic elansolid C1 (8) was isolated from Chitinophaga sancti strain FxGBF13 after fermentation in the presence of anthranilic acid. Remarkably, 8 was also obtained by addition of anthranilic acid to a crude fermentation extract containing the macrolide elansolid A2 (1*). This Michael-type conjugate addition allowed us to generate 21 new derivatives of elansolid C1 (9-29) by using various nucleophiles. Biological activities of all derivatives were evaluated against Staphylococcus aureus, Micrococcus luteus, and the mouse cell line L929.     

Inhibition of Human DHODH by 4‐Hydroxycoumarins,Fenamic Acids,and N‐(Alkylcarbonyl)anthranilic Acids Identified by Structure‐Guided Fragment Selection

A strategy that combines virtual screening and structure‐guided selection of fragments was used to identify three unexplored classes of human DHODH inhibitor compounds: 4‐hydroxycoumarins, fenamic acids, and N‐(alkylcarbonyl)anthranilic acids. Structure‐guided selection of fragments targeting the inner subsite of the DHODH ubiquinone binding site made these findings possible with screening of fewer than 300 fragments in a DHODH assay. Fragments from the three inhibitor classes identified were subsequently chemically expanded to target an additional subsite of hydrophobic character. All three classes were found to exhibit distinct structure–activity relationships upon expansion. The novel N‐(alkylcarbonyl)anthranilic acid class shows the most promising potency against human DHODH, with IC₅₀ values in the low nanomolar range. The structure of human DHODH in complex with an inhibitor of this class is presented.