蒎酮酰芳胺衍生物的合成

以α-蒎烯为原料、高锰酸钾为氧化剂合成了2-(3-乙酰基-2,2-二甲基环丁基)乙酸(即蒎酮酸).蒎酮酸与氯化亚砜反应生成酰氯,再与取代芳胺反应生成了8种可能具有生物活性的蒎酮酰芳胺衍生物,探讨了反应条件,并对产物进行了结构鉴定.     

蒎酮酰胺衍生物的合成

以α-蒎烯为原料、水为反应溶剂、高锰酸钾为氧化剂合成了2-(3-乙酰基-2,2-二甲基环丁基)乙酸(即蒎酮酸),蒎酮酸的收率为50%.蒎酮酸与氯化亚砜反应生成酰氯,再与取代芳胺反应生成了6种蒎酮酰胺衍生物,产品收率介于40.4%～69.9%之间.     

抗癫痫1,2,4-三氮唑类衍生物研究进展

根据含1,2,4-三氮唑结构单元化合物的结构特点,总结了并环类和非并环类抗癫痫药物活性方面的研究进展,重点分析了不同结构类型与其抗癫痫活性以及神经毒性之间的关系。得出结论,1,2,4-三氮唑并喹啉、喹唑啉衍生物和三氮唑硫酮衍生物因具有良好的活性、较低的毒性从而具有进一步研究和开发的价值;在此基础上,对1,2,4-三氮唑类化合物抗癫痫活性未来的研究方向进行了展望。     

三组分一锅合成1,4-苯并硫氮杂卓衍生物

苯并硫氮杂卓衍生物是一类重要的七元杂环化合物,有着重要的药理活性和生物活性,它的某些衍生物已经作为催眠药物、抗焦虑药物和心血管药物应用于临床。本文用4-氯苯甲醛、2-氨基苯硫酚和季酮酸为原料,二氯乙烷为溶剂,多组分反应一步合成三环1,4-苯并硫氮杂卓衍生物,实验产率高,条件温和。目标化合物的结构经红外光谱、氢谱、碳谱和高分辨质谱进行了表征。     

季酮酸中间体化合物的合成方法改进

季酮酸片段是螺环季酮酸类杀虫杀螨剂的重要的中间体。在现有工艺基础上,采用正丁基锂作为酯交换和环合的碱性试剂,一步制备该中间体,提高了该中间体收率,缩短反应时间,操作更加方便。本工艺适合产业化生产螺环季酮酸类杀虫杀螨剂中间体片段。     

PMNAP缩2-氨基苯并噻唑席夫碱及其过渡金属配合物的合成与抑菌活性

在非水溶剂中合成出一种未见报道的新型席夫碱试剂(HL):1-苯基-3-甲基4-萘乙酰基-吡唑啉酮-5(PMNAP)缩2-氨基苯并噻唑及其4种过渡金属配合物.由元素分析、化学方法、质谱和摩尔电导值推测出配合物的组成为ML·H2O[M=Cu2+、Pb2+、Ni2+、Zn2+],通过红外光谱、紫外光谱、热重谱和核磁共振氢谱等手段对配体和配合物进行了结构表征并做了初步的抑菌活性实验.表征结果显示:配体在测试条件下以酮式和烯醇式结构共存,配位时酮式可能转化为烯醇式结构按去质子的方式以1分子吡唑啉酮环羟基和1分子H2O上的两个0原子以及亚胺基和苯并噻唑环上的两个N原子与过渡金属中心离子成键,配合物的配位数为4;抑菌实验结果表明:配合物比配体对枯草杆菌、大肠杆菌、酵母菌和金黄色葡萄球菌具有更强的抑制作用.     

还原染料和防红外伪装性能

具有蒽醌、苯并蒽酮、吖啶稠环系列和分子中含有氧、硫的五元杂环结构的苯蒽酮衍生物和苯系衍生物结构的还原染料,具有对红外线有良好的吸收性生能,接近绿色树叶反射光谱曲线、波长在680 ～ 710nm的还原染料可适用防红外伪装.文中叙述了还原染料防红外反射的机理,防红外伪装的还原染料结构及用于防红外的还原染料.     

硼酸催化的一锅法合成3,4-二氢嘧啶-2-酮衍生物

以硼酸为催化剂,由芳香醛、β-酮酸酯和尿素合成了系列3,4-二氢嘧啶-2-酮衍生物.在无溶剂条件下回流反应1～2 h,反应产率可达73%～92%.产物结构经1HNMR、IR确证.该方法具有催化剂廉价易得,反应时间短,收率高,对环境友好等优点.     

4,5-二氢[1,2,4]三氮唑并[4,3-a]喹啉衍生物的合成

三氮唑环和喹啉酮环均为抗真菌药物的基本药效基团,为探索二氢喹啉酮并入三唑环对抗真菌活性的影响,设计并合成了7-氨基-4,5-二氢[1,2,4]三氮唑并[4,3-a]喹啉衍生物,其结构经质谱、红外光谱和核磁共振氢谱确证。     

螺甲螨酯合成工艺改进研究

<正>1前言螺甲螨酯(spiromesifen)是由拜耳公司开发的螺环季酮酸(具有环状酮-烯结构的氧代丁内酯)类杀虫、杀螨剂。其作用机理独特,通过抑制螨害体内的脂肪合成,破坏螨虫的能量代谢活动,最终杀死螨害。具有广谱、持效期长、毒性低、无交互抗性等特点,广泛应用于害虫、害螨的防治。螺甲螨酯的合成工艺路线比较单一,国内外目前一般都采取以环戊酮和氰化钠为起始原料制备中间体1-羟基环戊基甲酸乙酯(3),再与2,4,6-三甲基苯乙酰氯经缩     

螺环季酮酸衍生物的合成及生物活性研究

以螺螨酯类杀螨剂为先导,运用类同合成、生物电子等排理论,合成了28个螺环季酮酸类新化合物。通过1H NMR、IR和元素分析对所合成的化合物进行了结构确认。初步生物活性测试结果表明,在试验浓度下部分化合物具有很高的生物活性。     

Cyclic hydroxamic acid accumulation in corn seedlings exposed to reduced water potentials before,during, and after germination

Cyclic hydroxamic acids are innate compounds associated with pest resistance in several grass species. The major cyclic hydroxamic acids of com, 2,4-dihydroxy-7-methoxy-2H-1,4-benzoxazin-3-one (DIMBOA) and 2,4-dihydroxy-3H-1,4-benzoxazin-3-one (DIBOA), were measured in seedlings after exposure to various water stress treatments. Both DIMBOA and DIBOA were found in greater quantities in plants experiencing a water deficit stress than in nonstressed plants. The increased cyclic hydroxamic acid coincided with a reduction in seedling growth, suggesting that cyclic hydroxamic acids are stress metabolites. Plants grown under conditions that restrict growth, such as water deficit stress, contain higher cyclic hydroxamic acids, which should make them more resistant to herbivorous pests and pathogenic microorganisms.     

Using propylene carbonate in extraction and absorption: A review

Propylene carbonate is a cyclic alkyl carbonate (1,3-dioxolan-2-one, 4-methyl), soluble in alcohol, ether, acetone, aromatic hydrocarbons, and acetic acid and insoluble in aliphatic hydrocarbons and CS₂.     

Spiroheterocyclic system. Part IV: Novel azo dye sulpha drugs of spiroheterocyclic naphthenes

Novel azo-dyes have been synthesized by diazotization of 4-amino benzene-4′-(substituted heterocyclo) sulphonamide derivatives and coupling with 1-oxa-4-thia-spiro[4,4]nonan-2-one (I) and/or with l-oxa-4-thia-spiro[4,5]decan-2-one (I′) in acid medium to give the corresponding 3-azo-(4′-substituted benzenesulphonamido)-l-oxa-4-thia-spiro[4,4]nonan-2-one (II-IX) and/or l-oxa-4-thia-spiro[4,5]decan-2-one (II′-IX′] as spiro-ligands. Treatment of these ligands with metal salts of iron (Fe³⁺), copper (Cu²⁺) and mercury (Hg²⁺) as chlorides in ethanolic solution furnished the corresponding metal chelates (II_a-c-IX_a-c) and/or (II′_a-c-IX′_a-c). The compounds were tested in vitro for antimicrobial activity to study the structure-activity relationship.     

4-羟基-3-取代苯基-2H-苯并吡喃-2-酮衍生物的合成及杀菌活性

以水杨酸甲酯和取代苯乙酸为原料.经缩合、环化得到中间体4-羟基-3-取代苯基-2H-苯并吡喃-2-酮,与酰氯反应,合成了16个未见文献报道的4-羟基-3-取代苯基-2H-苯并吡喃-2-酮衍生物(3),所有目标化合物结构均通过1H NMR、IR和LC/MS确证.初步生物活性测试表明:在质量浓度25 mg/L下,化合物3k和30对黄瓜灰霉病菌抑制率分别为67.3%和73.9%;在质量浓度500 mg/L下,化合物3d、3k和3e对稻纹枯病菌的活性分别为75.0%、73.6%和100%.     

Synthesis and antimicrobial activity of some new 2-(3-chloro-1-benzothiophen-2-yl)-3-(substituted-phenyl)-4- (3H)-quinazolinones derivatives

3-Chloro-1-benzothiophene-2-carbonylchloride 1 reacted with anthranilic acid in pyridine to give compound 2. The main aim of the work is to study the behavior of this 4H-3,1-benzoxazin-4-one toward nitrogen nucleophiles. The compound reacted with aromatic amines, hydroxylamine hydrochloride, formamide, thioglycolic acid, thiosemicarbazide and acid chlorides to give various 3-substituted quinazolinones, respectively. The structures of all the synthesized compounds were confirmed by spectral data and have been screened for antibacterial and antifungal activity.

     

Electrochemical partial fluorination of organic compounds: 82: Anodic α-fluorination of five-membered cyclic thiocarbonates

Anodic fluorination of various kinds of five-membered cyclic thiocarbonates was carried out under various electrolytic conditions and the corresponding α-monofluorinated products were obtained in the cases of 1,3-oxathiolane-2-one and 1,3-dithiolane-2-one with high regioselectivity. On the contrary, oxidative desulfurization of cyclic thiocarbonates with a CS bond took place to provide the corresponding gem-difluorinated product and/or carbonyl compounds depending on the molecular structures of the starting thiocarbonates.     

季酮酸类杀虫杀螨剂品种及其合成方法

介绍了季酮酸类杀虫杀螨剂的开发进展以及这类化合物的作用机理和合成方法,特别是新杀虫剂螺虫乙酯,高效而新颖,必将在作物有害生物治理中发挥重要作用,具有良好的发展前景。     

Synthesis and antibacterial activity of thioglycolic amino acid derivatives and dipeptides containing the 2-methyl-3,4-dihydroquinazolin-4-one moiety

3-(2′-Chloroethyl)-2-methyl-3,4-dihydroquinazolin-4-one ( I ) was reacted with sodio (sodium thioglycolate) in dry dioxane and yielded compound II . By using thionyl chloride, this compound was converted to the corresponding acid chloride ( III ). The prepared acyl chloride ( III ) was allowed to interact with different α-amino acids such as Gly, L -Ala, L -B-Phe, DL -Asp, L -Glu, L -Thr and L -Val to give new amino acid derivatives ( IVa – g ). A selected C-terminal derivative of glycine ( IVa ) was converted into acid chloride ( V ). The acid chloride formed was reacted with L -Ala, L -B-Phe, DL -Asp, L -Glu, L -Thr and L -Val and yielded the new dipeptides VIa – f . The structures of the synthesized compounds were elucidated by elemental analysis and IR spectra. The prepared peptides were tested for their antimicrobial activities by comparison with tetra-cycline as a reference compound.     

Soil transformation of wheat and corn metabolites mboa and DIM2BOA into aminophenoxazinones

The defensive cyclic hydroxamates 7-methoxy-2,4-dihydroxy-1,4(2H)-benzoxazin-3-one (DIMBOA) and 7,8-dimethoxy-2,4-dihydroxy-1,4(2H)-benzoxazin-3-one (DIM₂BOA) of wheat and corn are transformed in nonsterile soil, via 6-methoxy-2(3H)-benzoxazolone (MBOA) and 6,7-dimethoxy-2(3H)-benzoxazolone (M₂BOA) respectively, into 2-amino-7-methoxy-3H-phenoxazin-3-one and 2-amino-4,6,7-trimethoxy-3H-phenoxazin-3-one. The soil transformation is similar of that undergone by the rye metabolite 2(3H)-benzoxazolone (BOA) into 2-amino-3H-phenoxazin-3-one. The transformations to phenoxazinones are not observed in sterile soil. The 2-amino-3H-phenoxazin-3-one inhibits barnyard grass radicle elongation, but the methoxylated aminophenoxazinones are not significantly inhibitory.