Long chain carboxylic acids containing ether linkage: V. N-methyl substituted glycine-type amphoterics containing alkoxy radical

The substituted glycine-type amphoteric surfactants containing long chain alkoxy and methylated amino groups, such as N-(2-alkoxyethyl)methylaminoacetic acids and (N-[2-alkoxyethyl]-N-[carboxymethyl] dimethylammonium) chlorides, or N-(N-[2-alkoxyethyl]-2-aminoethyl) aminoacetic acids were synthesized, and their growth inhibitory activities against g positive, g negative bacilli, and some fungi were studied. The effect of substitution of methyl groups upon the amino group of the long chain alkoxyaminoacetic acids on their antimicrobial activities was examined, and the increasing effect, due to methyl substitution, was confirmed. The introduction of an aminoethyl radical between the alkoxyethyl and amino radicals of the substituted glycines also increased their antimicrobial activities. Dimethylsubstituted betain-type amphoterics showed less antimicrobial activities than the corresponding glycinetype amphoterics. Moreover, aqueous solution of these substituted glycine-type amphoteric compounds showed better surface activities at pH 4.0, 10.0 than at neutral pH.     

Long-chain carboxylic acids containing ether linkage III. The antibacterial and antifungal activities of the amine salts of someB-alkoxypropionic acids

Octylamine, dodecylamine, octadecylamine and triethanolamine salts ofβ-dodecyloxy- andβ-tetradecyloxypropionic acids, without or with one and with two oxyethylene groups between the alkoxy group and the propionic acid group, were prepared and examined as the growth inhibiting agents againstStaphylococcus aureus andPenicillium. Some of them were also tested againstTrichophyton asteroides, T. interdigitale, T. granulosus, Epidermophyton floccosum andMicrosporum canis. The effects of the alkyloxy, oxyethylene and amine groups on antibacterial and antifungal activities were determined. The dodecyl radical was more potent than the tetradecyloxy radical. The enhancing effect of the oxyethylene group was obscure in the amine salts. The most effective amine was dodecylamine and its salt ofβ-dodecyloxypropionic acid showed almost the same effectiveness as that of its mercury salt againstTrichophyton. As for the soluble amine salts, it was confirmed that their surface activities had nothing to do with their antibacterial and fungicidal powers.     

Long-chain fatty acids containing ether linkage. I. The antibacterial and fungicidal activities of some new β-alkyloxypropionic acids and their methyl esters

β-Alkoxypropionic acids and their methyl esters were made with alkoxy groups ranging from C₄H₉O to C₁₈H₃₅O: R-O-CH₂CH₂COOH (CH₃). Methyl esters and acids were also made with one and with two oxyethylene groups between the alkoxy group and the propionic acid group: RO (CH₂ CH₂ O) n-CH₂CH₂ COOH(CH₃). The compounds were tested againstStaphylococcus aureus and againstPenicillium for growth inhibition. The optimum size of the alkoxy group appears to be R=C₁₂H₂₅. Oxyethylene groups enhanced the activity againstS. aureus, but had relatively little effect againstPenicillium.     

N-(2-氨基苯)-4-[N-(吡啶-3-甲氧基碳酰)氨甲基]苯甲酰胺的合成

以3—羟甲基吡啶为起始原料，采用1，1′—碳酰二咪唑(CDI)法合成中间体4—[N—(吡啶—3—甲氧基碳酰)氨甲基]苯甲酸，然后与氯甲酸乙酯及三乙胺反应，制得活性中间体，该活性中间体不经分离直接与邻苯二胺在室温条件下反应即得目标产物。经质谱、核磁和红外等鉴定了目标分子的结构。     

Electrodeposition of functionalized Pyrrole (N-[3-(dimethylpyridyl-2-yl)aminopropyl], N-(3-aminopropyl), N-(3-acetamidopropyl) and N-(2-cyanoethyl)) on Stainless Steel gauze for membrane preparation

The preparation of dense membranes for ion separation by the electropolymerization of functionalized pyrrole has been carried out using pyrrole monomers with complexing groups such as amino and bis pyridine. The synthesis conditions of polymer films depend mainly on the applied potential and electrolyte composition; for polymer films derived from pyrrole monomers bearing amino groups, the film synthesis has been achieved only in acid solution. The main results obtained for the electropolymerization of N-(2-cyanoethyl)pyrrole, N-(3-aminopropyl)pyrrole, N-(3-acetamidopropyl)pyrrole and N-[3-(dimethylpyridyl-2-yl)aminopropyl]pyrrole are compared and the experimental conditions for membrane preparation discussed. The thickness and the morphology of the supported conducting polymer membrane prepared at a constant potential depend on the precursor monomer used. The duration of electrolysis should be sufficient to cover the metallic support, particularly for the N-[3-(dimethylpyridyl-2-yl)aminopropyl]pyrrole polymer membrane.     

N-(3-二甲氨基)烷基丙烯酰胺的合成研究

N-（3-二甲氨基）烷基丙烯酰胺是一类常用化合物的统称,比较具有代表性的化合物是N—（3-二甲氨基、丙基丙烯酰胺（简称DMAPAA）,在常温下是流动性液体,为不饱和叔胺。DMAPAA主要用做聚合物的单体、油田注水剂、絮凝剂、造纸助剂、分散剂、涂料助剂、医药中间体等。由于其分子结构中存在着叔胺基团和乙烯基团．能形成季铵盐或发生聚合反应,具有如下特点：单体活性高、形成聚合物的相对分子质量大、呈碱性且显阳离子性、水溶性和醇溶解性都较好、能被广泛应用做石油污水处理和造纸废水处理的第四代絮凝剂单体、还可以用做石油和天然气三次开采的化学助剂单体等。但是,由于它的合成条件非常苛刻,国内还没有成熟的合成工艺条件及设备．主要依靠进口。目前世界上只有德国和日本的工厂具有较完善的合成工艺条件．对单体以及相关产品的研究和开发有较强的理论意义和应用价值。该产品在国内外都具有广阔的市场前景．对国家和企业都具有巨大的经济和社会效益．     

Poly[N-(2-hydroxypropyl)methacrylamide]. IV. Heterogeneous polymerization

Kinetics of radical heterogeneous polymerization of N-(2-hydroxypropyl)methacrylamide was studied in acetone at 55°C. The values of reaction order with respect to the monomer (1.6) and to the initiator (0.5) indicate a bimolecular termination and degradative transfer during the chain growth. The over-all rate constant of polymerization was found to be 5.6.10-4. Addition of a small amount of a solvent (methanol) to the polymerization mixture led to an increased polymerization rate and increased molecular weight of the resulting polymer, but a higher amount of the solvent brought about a decrease of both characteristics. The Occurence of maxima on the dependences of R_p, as well as M?_w on the monomer concentration was interpreted in terms of the classical Bamford and Jenkins theory.     

Design, synthesis, and in vitro antibacterial activity of fluoroquinolone derivatives containing a chiral 3-(alkoxyimino)-2-(aminomethyl)azetidine moiety

A series of novel (R)/(S)-7-(3-alkoxyimino-2-aminomethyl-1-azetidinyl)fluoroquinolone derivatives were synthesized and evaluated for their in vitro antibacterial activity against representative strains. Our results reveal that 12 of the target compounds generally show better activity (MIC: <0.008-0.5 μg mL(-1)) against the tested Gram-positive strains including MRSA and MRSE than levofloxacin (LVFX, MIC: 0.125-8 μg mL(-1)). Their activity is similar to that of gemifloxacin (GMFX, MIC: <0.008-4 μg mL(-1)). However, they are generally less active than the two reference drugs against Gram-negative strains. Moreover, against clinical strains of S. aureus including MRSA and S. epidermidis including MRSE, the MIC(50) values (0.06-16 μg mL(-1)) and MIC(90) values (0.5-32 μg mL(-1)) of compounds 16 w, y, and z are 2-8- and 2-16-fold less than LVFX, respectively, and 16 w (MIC(90) range: 0.5-4 μg mL(-1)) was also found to be more active than GMFX (MIC(90) range: 1-8 μg mL(-1)).     

3-溴-1-(3-氯-2-吡啶基)-1H-吡唑-5-甲酸的合成研究

3-溴-1-(3-氯-2-吡啶基)-1H-吡唑-5-甲酸是合成新型鱼尼丁受体杀虫剂氯虫酰胺(chlorantraniliprole)的关键中间体.以2,3-二氯吡啶为原料通过肼基取代、马来酸二乙酯环合、对甲基苯磺酰氯酯化、溴化氢溴化、浓硫酸氧化脱氢以及水解6步反应制得3-溴-1-(3-氯-2-吡啶基)-1H-吡唑-5-...     

去乙酰酶抑制剂N-(2-氨苯基)-4-[N-(吡啶-3-甲氧羰基)氨甲基]苯甲酰胺的合成

以3 羟甲基吡啶为起始原料,采用碳酰二咪唑(CDI)法在0～10℃下搅拌反应,合成中间体4 [N (吡啶 3 甲氧羰基)氨甲基]苯甲酸(Ⅰ),收率为83 9%;然后与氯甲酸乙酯及三乙胺在0～10℃下搅拌反应,制得酸酐活性中间体(Ⅱ);它不经分离直接与邻苯二胺在室温条件下反应10h即得目标产物:N (2 氨苯基) 4 [N (吡啶 3 甲氧羰基)氨甲基]苯甲酰胺,经硅胶柱层析提纯后,收率为45 0%,总收率为37 8%,合成具有一定绿色化学特性;经质谱、核磁和红外等谱学方法鉴定了目标分子结构。     

New amphoteric surfactants containing a 2-hydroxyalkyl group: I preparation and properties of N-(2-hydroxyethyl)-N-(2-hydroxyalkyl)-β-alanines

A series of new amphoteric surfactants, sodium salts of N-(2-hydroxyethyl)-N-(2-hydroxyalkyl)-β-alanines (Na-HAA) was prepared by adding methyl acrylate to N-(2-hydroxyalkyl)-ethanolamine and subsequent saponification. Neutralization with HCl gave N-(2-hydroxyethyl)-N-(2-hydroxyalkyl)-β-alanines, and the addition of ethylene oxide to Na-HAA gave oxyethylated drivatives. The structures of these compounds prepared were confirmed by infrared spectra, proton magnetic resonance spectra, elementary analyses, etc. Solubility in water, surface tension, foaming power, and critical micelle concentration were determined.     

N-(取代苯氧乙酰基)-3-氨基-二氢噻吩-2-酮衍生物的合成和生物活性

酰胺类化合物具有很高的药用活性,为了进一步研究酰胺衍生物的合成与性质,文中用3-氨基-二氢噻吩-2-酮盐酸盐与取代苯氧乙酸反应,得到N-(取代苯氧乙酰基)-3-氨基-二氢噻吩-2-酮衍生物。产物结构经IR、1H NMR和元素确证。对5种病原菌的抑菌活性进行了生物活性测试。合成中采用三氯氧磷为缩合试剂,采用一锅反应,简便易行,缩合试剂价廉易得、反应收率高,产物纯度较高,为此类新化合物的合成和筛选提供了依据。     

The STOBBE condensation. XI. The cyclisation of (Z)- and (E)-3-methoxycarbonyl-2-methyl-4-(2′-naphthyl)-4-phenyl-but-3-enoic acids to the corresponding polysubstituted phenanthrene and naphthalene derivatives

(Z)- and (E)-3-methoxycarbonyl-2-methyl-4-(2′-naphthyl)-4-phenyl-but-3-enoic acids 1 a and 4 a have been converted into methyl-4-acetoxy-3-methyl-1-phenylphenanthrene-2-carboxylate 2 a and methyl 4-acetoxy-3-methyl-1-(2′-naphthyl)-2-naphthoate 5 a . The derived phenolic acids 2 b and 5 b are converted to methyl 4-methoxy-3-methyl-1-phenyl-phenanthrene-2-carboxylate 2 c and methyl 4-methoxy-3-methyl-1-(2′-naphthyl)-2-naphthoate 5 c ; which are saponified to the corresponding methoxy acids 2 d and 5 d . Alcoholysis of the anhydrides 3 and 6 gives the corresponding half-esters 1 c and 4 c , respectively.     

N-（2-（7-氯-4-氧代-2-苯氨基喹唑啉-3（4H）-基）乙基）酰胺的合成

研究了N-（2-（7-氯-4-氧代-2-苯氨基喹唑啉-3（4 H）-基）乙基）酰胺的合成方法。以4-氯-2-氨基苯甲酸为起始原料,通过氮杂-Wittig反应合成关键中间体7-氯-3-氨乙基-2-苯氨基喹唑啉酮,再以酰胺类似物为先导,根据活性亚结构拼接原理,将活性基团喹唑啉酮乙基导入酰胺基中,设计合成一系列含喹唑啉酮乙基的新型酰胺类似物,并通过IR、1 HNMR、MS及元素分析等对其结构进行确证。     

N-(p-溴苯基)-2-(p-氯苯氧乙酰基)氨基脲的合成与表征

用 Ｎ － （ｐ － 溴苯基） 三氯乙酰胺与ｐ － 氯苯氧乙酰肼反应,合成了一种新的取代氨基脲, Ｎ － （ ｐ － 溴苯基） － ２ － （ ｐ － 氯苯氧乙酰基） 氨基脲,其结构经 Ｉ Ｒ 、１ Ｈ Ｎ Ｍ Ｒ 和元素分析证实。     

N-(2-羟乙基)-2-噁唑烷酮的合成及应用

通过均匀设计实验,二乙醇胺与碳酸二甲酯反应合成了硼酸酯键合剂中间体N-(2-羟乙基)-2-噁唑烷酮;用SPSS软件处理实验数据,确定了合成N-(2-羟乙基)-2-噁唑烷酮收率与各反应因素的回归方程。得到其最优反应条件为碳酸二甲酯与二乙醇胺摩尔比:1.3∶1,催化剂甲醇钠的质量占二乙醇胺质量的0.50%,反应温度60℃,反应时间60 min;在该条件下,N-(2-羟乙基)-2-噁唑烷酮收率达98.2%。以N-(2-羟乙基)-2-噁唑烷酮和二乙醇胺共混合成的硼酸酯键合剂(BEBA)以相同的工艺和配方应用于5 L丁羟四组元推进剂装药实验,结果显示:推进剂常温、高温各项力学性能指标均高于发动机设计要求15%,高温黏附指数φ为1.02,其综合力学性能优于醇胺类键合剂LAB-303B、二乙醇胺硼酸酯键合剂BAG-5及海因三嗪类键合剂BA603。     

3-[N-(3-烷氧基-2-羟基丙基)-N,N-二甲基铵]-2-羟基丙基酸性磷酸酯甜菜碱的合成

以高级脂肪醇、环氧氯丙烷、二甲胺和磷酸二氢钠为原料,合成了一类新型的磷酸酯甜菜碱两性表面活性剂3-[N-(3-烷氧基-2-羟基丙基)-N,N-二甲基铵]-2-羟基丙基酸性磷酸酯甜菜碱(简称AHDHPB),并通过红外光谱对其结构进行了分析,测定了表面活性。研究了AHDHPB．12和阴离子表面活性剂(As)复配体系的降低表面张力能力、降低表面张力效率的增效作用。结果表明,合成的两性表面活性剂AHDHPB结构独特,具有较高活性和复配性能。     

The N-(2-carboxyphenyl)salicylideneimine ligand in 4f-metal chemistry: A unique neodymium(III) chain containing the singly deprotonated,zwitterionic form of the ligand

The reactions of N-(2-carboxyphenyl)salicylideneimine and hydrated praseodymium(III) or neodymium(III) chlorides give 1D complexes with interesting structural and spectroscopic features; the chains possess the singly deprotonated ligand which is in its zwitterionic form.