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Boron trifluoride etherate in organic synthesis 有机合成中的三氟化硼醚
Pub Date : 2019-01-21 DOI: 10.15406/MOJBOC.2019.03.00090
A. K. Banerjee, Alexis Maldonado, D. Arrieche, W. Vera, Elvia V. Cabrera, P. Poon, Liadis Bedoya
The innumerable applications of boron trifluoride etherate of boron trifluoride etherate in organic synthesi1,2 encouraged us to write a micro review on this reagent. The commercially available boron trifluoride etherate (b.p. 126oC), a brown liquid, is very toxic by inhalation, causes severe burns, reacts violently with water, hot alkali or alkaline earth (not Mg) metals with incandescence. It can be purified by distillation. This review would discuss only four principal use of boron trifluoride etherate: (a) hydroboration–oxidation reaction, (b) cleavage and rearrangement of epoxides, (c) esterification (d) cyclization. In addition, some other minor uses of boron trifluoride etherate will be briefly described.
三氟化硼醚在有机合成中的无数应用1,2促使我们对该试剂进行微综述。市售的三氟化硼醚(b.p.126oc)是一种棕色液体,吸入后毒性很大,会引起严重烧伤,与水、热碱或碱土(不是Mg)金属发生剧烈反应,会发出白炽。它可以通过蒸馏提纯。本综述将只讨论三氟化硼醚的四种主要用途:(a)硼氢化氧化反应,(b)环氧化物的裂解和重排,(c)酯化(d)环化。此外,还将简要介绍三氟化硼醚的其他一些次要用途。
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引用次数: 4
Catalytic activity of graphene oxide hybridized ZnWO4 for dyes degradation and oxidation of functionalized benzyl alcohols 氧化石墨烯杂化ZnWO4对染料降解和官能化苯甲醇氧化的催化活性
Pub Date : 2018-10-29 DOI: 10.15406/MOJBOC.2018.02.00087
Ajay Kumar Paliki, S. Botsa, Sailaja Bbv
Recently, nanomaterials have great attention due to their unique size, shape, and crystallinity dependent optical, electronic, magnetic and chemical properties.1 Metal tungstates such as. Bi2WO6, CdWO4, PbWO4, MnWO4 and FeWO4 are inorganic functional nanomaterials and widely used in scintillators materials, sensors, magnetic devices, photocatlaytic and magnetism field.2 Among them, ZnWO4 has a great potential in photocatalytic degradation of organic dye pollutants under UV light illumination.2−3 But, the efficiency is very low because of sunlight captures only 5% while visible light captures the 35%. Hence, this material activity brings to visible region by doping of ions, form hybrids or composites with graphene or CNT. Graphene is a sp2 hybridized carbon with zero band gap energy and has specific physicochemicoelectrical properties thus it shows excellent applications in photocatalysis and organic conversions.4 There have been persistent efforts to load photocatalysts on the structure of graphene oxide (GO) to enhance the photo catalytic activity, but few studies have focused on the surface coating by GO on the photcatalyst for enhancing the photo catalytic efficiency and producing visible photocatalytic activity.
近年来,纳米材料因其独特的尺寸、形状和结晶度对光学、电子、磁性和化学等方面的影响而受到人们的广泛关注金属钨酸盐,如。Bi2WO6、CdWO4、PbWO4、MnWO4和FeWO4是无机功能纳米材料,广泛应用于闪烁体材料、传感器、磁性器件、光催化和磁场等领域其中,ZnWO4在紫外光照射下光催化降解有机染料污染物方面具有很大的潜力。但是,效率很低,因为太阳光只捕获了5%,而可见光捕获了35%。因此,通过掺杂离子,与石墨烯或碳纳米管形成杂化或复合,将这种材料的活性带到可见区域。石墨烯是一种带隙能为零的sp2杂化碳,具有特殊的物理化学和电学性质,因此在光催化和有机转化方面具有良好的应用前景人们一直致力于在氧化石墨烯(GO)结构上负载光催化剂以提高光催化活性,但很少有研究关注氧化石墨烯在光催化剂表面涂覆以提高光催化效率并产生可见光催化活性。
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引用次数: 3
Reaction of o-bromoaryl- and o-bromoarylalkyl phthalimides with n-butyllithium at low temperatures 邻溴芳基和邻溴芳基烷基酞酰亚胺与正丁基锂的低温反应
Pub Date : 2018-10-17 DOI: 10.15406/mojboc.2018.02.00086
David A Hunt
The work of Parham, Jones and Sayed,1 which demonstrates that bromine-lithium exchange, occurs in preference to carbonyl addition in aromatic amide derivatives of o-bromo-β-phenylpropionic acid, led to the consideration of using o-bromoaryl phthalimides 1a-c as precursors for the preparation of multi-ring nitrogen heterocycles and for elaborations of aromatic systems requiring an amine-protecting group (Figure 1). While the chemistry of the addition of Grignard and organolithium reagents to phthalimides is well known,2 to the best of our knowledge, attempts to carry out the addition of the these reagents to brominated phthalimide derivatives such as 1a-c have not been studied.
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引用次数: 1
Roles of metals in human health 金属在人体健康中的作用
Pub Date : 2018-09-19 DOI: 10.15406/mojboc.2018.02.00085
Satya P Gupta
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引用次数: 2
Benzylation of 1,3-diketons in the phase transfer catalysis condition by microwave irradiation 微波相转移催化条件下1,3-二酮的苄基化反应
Pub Date : 2018-09-05 DOI: 10.15406/mojboc.2018.02.00084
Torosyan Gh, Hovhannisyan Nr
1,3-diketones as ethyl acetoacetate (EAA) and diethyl malonate (DEM) are widely used to obtain a wide range of highly effective excipients in fine organic synthesis, specially for pharmaceutical industry. Microwave (MW) radiation exposure can significantly speed up reactions and increase the exit of the targeted materials, reducing the resorption in organic synthesis. MW radiation is a crucial tool for the development of green chemistry. Advantages of this method are lack of heat, cleanliness of the reaction, practical instantaneous heating of the reaction mass to the given temperature and, in particular, replacing the traditional solvent with an elevated and polar solvent.1,2 In this presentation have comprised the studied technique of alkylation in the usual phase transfer catalysis (PTC) in the same PTC condition with the combination of MW technique for the choice more convenient conditions for this important product synthesis. It is had been known, that the combination of the MW–PTC techniques was used in the alkylation of active methylene containing substrates such as ethyl acetoacetate.3
1,3-二酮类化合物作为乙酸乙酯(EAA)和丙二酸二乙酯(DEM)在精细有机合成中被广泛用于获得各种高效赋形剂,特别是在制药工业中。微波(MW)辐射暴露可以显著加快反应速度,增加目标物质的出口,减少有机合成中的吸收。毫瓦辐射是发展绿色化学的重要工具。该方法的优点是不需要热量,反应清洁,可以将反应质量瞬间加热到给定的温度,特别是可以用高极性溶剂代替传统的溶剂。本文介绍了在相同的相转移催化条件下,常用相转移催化(PTC)中烷基化反应的研究方法,并结合MW技术为这一重要产物的合成选择了更方便的条件。众所周知,MW-PTC技术的组合用于含活性亚甲基的底物如乙酰乙酸乙酯的烷基化
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引用次数: 0
A facile pseudo three component reaction for the synthesis of benzo [4,5]imidazo[1,2-a]pyridine derivatives 合成苯并[4,5]咪唑[1,2- A]吡啶衍生物的简易伪三组分反应
Pub Date : 2018-08-15 DOI: 10.15406/mojboc.2018.02.00083
Gnanasamb, Amirthalingam Vasuki, N. Nithya
The benzimidazole moiety is amongst the diversely active scaffolds as antifungal, antibacterial, antiviral, anticancer and antimalarial agents.1‒4 Therefore, developing new approaches towards the synthesis of benzimdazole fused heterocycles have always been on need.5 Also, indeno and isoquinolino fused heterocycles have gained greater attention because of their medicinal and synthetic importance over years and the broad range of biological activity.6‒8 Therefore, benzimidazole fused indene, pyridine or isoquinoline are of great interest in general and many synthetic procedures are available till date.1 Moved by these results we desired to achieve a facile general synthetic protocol to obtain these diverse molecules. Multicomponent reaction has always proved to be a versatile tool towards the synthesis of structurally diverse and complex heterocycles in simple one pot manner.9 Our research group is actively engaged in developing multi-component reaction protocols for the synthesis of skeletally diverse, functionalized and biologically relevant small heterocyclic hybrids.10‒12 We report a simple and rapid procedure for the preparation of benzo[4,5]imidazo[1,2a]pyridines (Figure 2) with 2-(1H-benzo[d]imidazol-2-yl)acetonitrile.
苯并咪唑部分是作为抗真菌、抗菌、抗病毒、抗癌和抗疟疾剂的多种活性支架之一。因此,开发苯并咪唑类杂环化合物的合成新方法一直是迫切需要的近年来,吲哚和异喹啉类杂环化合物因其广泛的生物活性以及在医学和合成方面的重要性而受到越来越多的关注。6-8因此,苯并咪唑融合茚、吡啶或异喹啉通常引起人们极大的兴趣,迄今已有许多合成方法受到这些结果的感动,我们希望实现一种简单的通用合成方案来获得这些不同的分子。多组分反应一直被证明是用简单的一锅法合成结构多样、复杂的杂环化合物的万能工具我们的研究小组积极致力于开发多组分反应方案,用于合成骨架多样化,功能化和生物相关的小杂环杂化物。我们报道了一种用2-(1h -苯并[d]咪唑-2-基)乙腈制备苯并[4,5]咪唑[1,2a]吡啶(图2)的简单快速方法。
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引用次数: 0
Design and synthesis of Azolidinedione/Thiazolidinediones teth-ered benzo[f]chromene derivatives and there in silico evaluation as tubulin inhibitors 偶氮烷二酮/噻唑烷二酮对端苯并[f]铬衍生物的设计合成及微管蛋白抑制剂的硅评价
Pub Date : 2018-08-08 DOI: 10.15406/mojboc.2018.02.00081
G. Vasuki
The small molecules that target microtubules is an attractive and an active area in cancer drug discovery.1‒4 These molecules bind to the tubulin, an α, βheterodimer and disrupt the dynamics of microtubule. Microtubule targeting agents can be classified into two categories. Microtubule stabilizing agents such as paclitaxel, docetaxel, epothilones, and discodermolide binds to the tubulin polymer and stabilize the microtubules. Microtubule destabilizing agents such as vinca alkaloids, colchicine and combretastatins binds to tubulin dimers and cause destabilization.5 The equilibrium between tubulin and microtubule is altered, which results in disruption of mitotic spindle. This effects a critical transition in the cell cycle, leading to cell death. Out of these different pockets on tubulin, colchicine is a significant source of inspiration for the design of new drugs as the colchicine binding site inhibitors binds with high affinity at the interface of α and β-tubulin. These are effective against multidrug mechanisms but however, the potential clinical applications of colchicine site tubulin inhibitors have been nullified by the significant toxicities against the normal cells, low solubility, and low bioavailability.6,7 The increase in resistance of cancer cells against current clinical drugs and poor tolerance of the existing anticancer drugs, intensifies the need to identify new molecules as anticancer drugs with high potency, minimal side effects.
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引用次数: 1
Biodegradable polymers for sustainable environmental and economic development 生物可降解聚合物的可持续环境和经济发展
Pub Date : 2018-08-06 DOI: 10.15406/mojboc.2018.02.00080
I. Shamsuddin, Sani N, A. M, A. Mk
The alarming awareness related to environmental and waste management issues around the universe, status and negative effects of fossil resources, are some of the reasons why biodegradable polymers and the need for their usage is increasingly promoted for sustainable development. Moreover, there is no sustainable economic development without a sustainable environment. Researchers universally have proven that fossil resources pose a serious threat to existence of humans, plants and animals by the generation of greenhouse gases and CFC’s. Critically observing the scenario, there is no need to exaggerate the importance of the safe and healthy environment to universal sustainable development. It is a prerequisite on which human and other living things existence lies. Biodegradable biopolymers from research results do not pose such a threat to the environment and its inhabitants compared to fossil based polymers, and therefore, there is need for biodegradable biopolymers universally. Abaza et al., cited in Pathak et al.1 opined that any global scheme of development created without taking the environment into account will actually be a house built on sand.
人们对世界各地的环境和废物管理问题、矿物资源的现状和负面影响的惊人认识,是日益促进可持续发展的可生物降解聚合物及其使用需求的一些原因。此外,没有可持续的环境,就没有可持续的经济发展。研究人员普遍证明,化石资源通过产生温室气体和氯氟烃对人类、植物和动物的生存构成严重威胁。仔细观察这一情况,没有必要夸大安全和健康环境对普遍可持续发展的重要性。它是人类和其他生物存在的先决条件。与化石基聚合物相比,研究结果表明可生物降解的生物聚合物不会对环境及其居民构成威胁,因此,普遍需要可生物降解的生物聚合物。Pathak et al.1中引用的Abaza等人认为,任何不考虑环境的全球发展计划实际上都是建在沙子上的房子。
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引用次数: 20
Assessment of the level of seminal zinc and fructose concentration in seminal plasma of Vietnamese infertile men 越南不育男性精浆中精锌和精果糖浓度的评价
Pub Date : 2018-08-03 DOI: 10.15406/MOJBOC.2018.02.00079
N. Trang, Trieu Tien Sang, N. Hoang, N. G. Khanh, Tran Trung Duc
Infertility is defined as the failure of a couple to achieve a pregnancy after at least one year of frequent unprotected intercourse.1,2 It has been reported that the male partner contributes in 40% of the cases of infertility. Globally, the incidence of fertility is estimated to be about 13-18%.1,3 Due to the various reasons caused male infertility, it is essential to identify appropriate diagnosis methods to detect them. There are many tests that have been applied for several decades such as semen analysis, genetic tests and hormones methods. Recently, some of biochemical markers including zinc and fructose are becoming significant implications for diagnosing the cause in male infertility.4 They have thus been established as good indicators of human male fertility. An understanding of the factors affecting these characteristics is critical to proper understanding of the mechanisms underlying male infertility.5,6 Fructose is essential for spermatozoa metabolism and spermatozoa motility.7 Fructose is an energy source for spermatozoa. It is produced by the seminal vesicles with some contribution from the ampulla of the ductus deferens.8,9 Determination of seminal fructose concentration has been used in examination of obstructive azoospermia and inflammation of male accessory glands.10,11 The role of fructose concentrations in seminal plasma for total and sperm density has been investigated by several authors. Rajalakhshmi M, et al.,12 and Gonzales13 reported that an increase in sperm concentration is often accompanied by a decrease in fructose concentration in seminal plasma, because sperm using fructose as the primary source of energy,12,13 However, others studies have also shown that fructose concentrations in seminal plasma of patients with oligozoospermia and azoospermia did not decrease as compared to normal men.
不孕症的定义是一对夫妇在至少一年的频繁无保护性交后未能怀孕。据报道,40%的不孕症病例是男性伴侣造成的。在全球范围内,生育率估计约为13-18%。1、3由于男性不育症的原因多种多样,确定合适的诊断方法来发现它们至关重要。有许多测试已经应用了几十年,如精液分析,基因测试和激素方法。近年来,锌、果糖等生化指标对男性不育的病因诊断具有重要意义因此,它们已被确定为人类男性生育能力的良好指标。了解影响这些特征的因素对于正确理解男性不育症的机制至关重要。果糖是精子代谢和精子活力所必需的果糖是精子的能量来源。它是由精囊产生的,并有一部分来自管壶腹。8,9精液果糖浓度的测定已被用于检查阻塞性无精子症和男性副腺炎症。一些作者已经研究了精浆中果糖浓度对总密度和精子密度的影响。Rajalakhshmi M等人12和gonzales等人13报道,精子浓度的增加往往伴随着精浆中果糖浓度的降低,因为精子以果糖作为主要能量来源12,13然而,其他研究也表明,少精症和无精症患者的精浆中果糖浓度与正常男性相比并没有降低。
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引用次数: 4
Biochemical reactions for the removal of heavy metals from aqueous solutions 从水溶液中去除重金属的生化反应
Pub Date : 2018-07-16 DOI: 10.15406/MOJBOC.2018.02.00078
Maher Mohamed Abed El-Aziza, Mohamed Ammar Khalifab
Olea europaea and Citrus aurantium are wild plants distributed in the Mediterranean region and grown since ancient time. Leaves of Olea europaea and Citrus aurantium contain so many biologically active ingredients such as fats/lipids, saponin, flavonoids, terpenoids etc. Occasionally, saponin was considered as a biological naturally occurring plant glycoside, characterized by their strong foaming properties in an aqueous solution that can be used as a ligand for decontamination of aqueous solutions due to its ability to form chemical complexes with heavy metals.1,2 Also, saponin has been applied as a surfactant having the complex-forming ability for determination of iron spectrophotometrically.3 The surfactant properties of saponin have been utilized as an important agent for heavy metal removal from aqueous wastes and remediation of contaminated sites. According to modern literature, saponins have served as a natural chelating agent to eliminate problems due to several heavy metals such as Cr, Cd, Cu, Pb, Zn, and As from soil and wastewater.4‒7 It has been shown that heavy metals were retained from its original solution due to some form of complexation with a carboxyl group (-COOH) in saponin.8 From a chemical point of view, the biochemical reaction between heavy metals and saponin represents a modern approach to (1) the synthesis of new organometallic complexes; (2) decontamination of industrial and radioactive effluents; (3) a non-traditional method for isolation of saponin from the plant kingdom. Our previous studies1 prove the presence of an oleanolic acid or hederagenin as an aglycone of triterpenoid saponin in Olea europaea and Citrus aurantium leaves as shown as in Figure 1. This means that there are at least two active centers (-OH and –COOH groups) coordinated directly with heavy metal atoms forming a complex. The concentration of the heavy metal, the concentration of saponin extract and pH were found the chemical operational variables affecting the biochemical reaction between saponin and heavy metal containing aqueous solutions. The present work aimed firstly to evaluate the biochemical reactions between saponin extracted from Olea europaea and Citrus aurantium leaves and lead/cadmium aqueous solutions under different physical environments. The effects of temperature, agitation, and synergism between them are the main operating factors under investigation affecting the reaction. Secondly, physicochemical characteristics of Olea europaea and Citrus aurantium leaves were determined to ensure the presence of a structure-behavior relationship.
欧洲油橄榄(Olea europaea)和柑橘(Citrus aurantium)是分布在地中海地区的野生植物,自古以来就有种植。油橄榄和金柑叶含有丰富的生物活性成分,如脂肪/脂质、皂苷、黄酮类化合物、萜类化合物等。偶尔,皂苷被认为是一种天然存在的生物植物糖苷,其特点是在水溶液中具有强烈的泡沫特性,由于其与重金属形成化学配合物的能力,可以用作水溶液净化的配体。此外,皂苷已被用作表面活性剂,具有络合物形成能力,用于分光光度法测定铁皂苷的表面活性剂特性已被广泛应用于废水中重金属的去除和污染场地的修复。根据现代文献,皂苷作为一种天然螯合剂,可以消除土壤和废水中铬、镉、铜、铅、锌、砷等重金属的污染。研究表明,由于与皂苷中的羧基(-COOH)的某种形式的络合作用,重金属被保留在原始溶液中从化学角度看,重金属与皂苷之间的生化反应代表了一种现代途径:(1)合成新的有机金属配合物;(二)工业污水和放射性污水的净化;(3)一种从植物界分离皂素的非传统方法。我们之前的研究1证明了在油橄榄和金柑橘叶片中存在齐墩果酸或异黄酮苷元作为三萜皂苷元,如图1所示。这意味着至少有两个活性中心(-OH和-COOH基团)与重金属原子直接配位形成配合物。发现重金属浓度、皂苷提取物浓度和pH是影响皂苷与重金属水溶液生化反应的化学操作变量。本文首先研究了不同物理环境下油橄榄和金柑叶中提取的皂苷与铅/镉水溶液的生化反应。温度、搅拌和协同作用是影响反应的主要操作因素。其次,测定了油橄榄和金柑橘叶片的理化特性,以确定两者存在结构-行为关系。
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引用次数: 3
期刊
MOJ Bioorganic & Organic Chemistry
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