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Synthesis and Biological Evaluation of 4-(3-Hydroxy-benzofuran-2-yl)coumarins 4-(3-羟基-苯并呋喃-2-基)香豆素的合成及生物学评价
Pub Date : 2014-03-27 DOI: 10.1155/2014/297586
Puttaraju Boregowda, Shivashankar Kalegowda, V. Rasal, J. Eluru, Ebenezer Koyye
Various 4-bromomethylcoumarins (1a-k) were reacted with methyl salicylate to yield 2-(2-oxo-2H-chromen-4-ylmethoxy)-benzoic acid methyl esters (2a-k). Formations of (3a-k) were achieved by using DBU under microwave irradiation. Structures of all the compounds were established on the basis of their spectral data. All the compounds were tested in vitro for their antimicrobial activity and cell cytotoxicity. All the tested compounds (2b-k) and (3a-k) were shown to be better activity against Staphylococcus aureus than the standard Ciprofloxacin. The compound (3k) (R = 6-OMe) was found to be more potent cytotoxic than the standard 5-fluorouracil.
不同的4-溴甲基香豆素(1a-k)与水杨酸甲酯反应得到2-(2-氧- 2h -铬-4-基甲氧基)苯甲酸甲酯(2a-k)。DBU在微波照射下形成(3a-k)。所有化合物的结构都是根据它们的光谱数据确定的。对所有化合物进行了体外抗菌活性和细胞毒性试验。所有被测试的化合物(2b-k)和(3a-k)对金黄色葡萄球菌的活性都比标准环丙沙星更好。发现化合物(3k) (R = 6-OMe)比标准的5-氟尿嘧啶具有更强的细胞毒性。
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引用次数: 8
Microwave Assisted Solvent-Free Synthesis of Some Imine Derivatives 一些亚胺衍生物的微波辅助无溶剂合成
Pub Date : 2014-03-26 DOI: 10.1155/2014/816487
Yunus Bekdemir, Kürşat Efil
Some imine derivatives (1a–7d) were synthesized using a rapid and an environmentally friendly method with reaction of aromatic aldehydes (a–d) and aromatic amines (1–7) (in 1 : 1 molar ratio) in the presence of -ethoxyethanol as a wetting reagent (2 drops) under solvent-free conditions using microwave heating.
以-乙氧基乙醇为润湿剂(2滴),在无溶剂条件下微波加热,以芳香醛(a - d)和芳香胺(1 - 7)(1:1摩尔比)反应合成了一些亚胺衍生物(1a-7d)。
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引用次数: 20
Synthesis of N-Alkyl-2-thiomethyl Benzimidazoles: A Green Approach n -烷基-2-硫甲基苯并咪唑的绿色合成方法
Pub Date : 2014-03-17 DOI: 10.1155/2014/239710
S. Rao, C. V. Reddy, P. K. Dubey
A green approach for the synthesis of N-alkyl-2-thiomethyl benzimidazoles 2 (R=CH3, C2H5, CH2Ph) under different conditions has been developed from N-alkyl-2-chloromethyl benzimidazole (i.e., CH3, C2H5, CH2Ph) 1 by reaction with thiourea by physical grinding, or by using green solvents like ethanol and PEG-600, or by using microwave irradiation technique.
以n -烷基-2-氯甲基苯并咪唑(即CH3, C2H5, CH2Ph) 1为原料,采用物理研磨法与硫脲反应,或采用乙醇、PEG-600等绿色溶剂,或采用微波辐照技术,建立了不同条件下合成n -烷基-2-硫甲基苯并咪唑2 (R=CH3, C2H5, CH2Ph)的绿色途径。
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引用次数: 0
An Efficient One-Pot Multi-Component Synthesis of 3,4-Dihydropyrimidin-2-(1H)-Ones/Thiones Catalyzed by Bismuth (III) Sulfate Trihydrate under Solvent-Free Conditions 无溶剂条件下三水合硫酸铋催化一锅多组分高效合成3,4-二氢嘧啶-2-(1H)-酮/硫酮
Pub Date : 2014-03-13 DOI: 10.1155/2014/761209
F. Hatamjafari
A convenient and efficient protocol for the one-pot synthesis of 3,4-dihydropyrimidin-2-(1H)-one/thione derivatives of aldehydes, and 1,3-dicarbonyl compounds with Bismuth (III) sulfate trihydrate as the catalyst was described. We had the advantages of good performance, simplicity, and short time reaction under solvent-free conditions. The catalyst can be repeatedly reused without loss of its activity.
介绍了一种以三水合硫酸铋为催化剂,一锅法合成3,4-二氢嘧啶-2-(1H)- 1 /硫酮醛衍生物和1,3-二羰基化合物的简便高效方法。该方法在无溶剂条件下具有性能好、操作简单、反应时间短等优点。该催化剂可重复使用而不丧失活性。
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引用次数: 5
Catalytic Synthesis of -Aminonitriles Using Nano Copper Ferrite under Green Conditions 绿色条件下纳米铁氧体铜催化合成-氨基腈
Pub Date : 2014-03-12 DOI: 10.1155/2014/169803
A. Gharib, N. Pesyan, L. V. Fard, M. Roshani
Copper ferrite nanomaterial as reusable heterogeneous initiator in the synthesis of α-aminonitriles. The nanocatalyst is easily recovered and its reusability is recorded. Synthesis of α-aminonitriles derivatives by one-pot reaction of different aldehydes with amines and trimethylsilyl cyanides has been developed using nano copper ferrite catalyst under room temperature and green solvent (water as solvent) conditions. α-aminonitriles are important in preparing a wide variety of amino acids, amides, diamines, and nitrogen containing heterocycles.
铁氧体铜纳米材料作为可重复使用的非均相引发剂在α-氨基腈合成中的应用。纳米催化剂易于回收,并记录了其可重复使用性。研究了以纳米铁氧体铜为催化剂,在室温和绿色溶剂(水为溶剂)条件下,不同醛类与胺类和三甲基硅氰化物一锅反应合成α-氨基腈衍生物。α-氨基腈在制备各种氨基酸、酰胺、二胺和含氮杂环中起着重要作用。
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引用次数: 10
One-Pot Synthesis of Metallopyrazinoporphyrazines Using 2,3-Diaminomaleonitrile and 1,2-Dicarbonyl Compounds Accelerated by Microwave Irradiation 微波加速2,3-二氨基马来腈和1,2-二羰基化合物一锅法合成金属吡嗪卟啉类化合物
Pub Date : 2014-02-27 DOI: 10.1155/2014/958951
A. Maleki, A. Rezayan
A one-pot microwave-assisted synthesis of metallopyrazinoporphyrazines as porphyrazine derivatives carrying six-membered pyrazine rings annulated at the periphery of the tetrapyrrolic macrocycle is described starting from 2,3-diaminomaleonitrile, 1,2-dicarbonyl compounds, metal salts, and urea.
以2,3-二氨基马来腈、1,2-二羰基化合物、金属盐和尿素为起始原料,微波辅助一锅法合成金属吡嗪卟啉衍生物,该卟啉衍生物携带六元吡嗪环,环在四吡啶大环的外围。
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引用次数: 5
In Quest of “Stereoselective Switch” for On-Water Hydrothiolation of Terminal Alkynes Using Different Additives and Green Synthesis of Vicinal Dithioethers 不同添加剂对末端炔在水中加氢硫基化的“立体选择开关”探索及邻二硫醚的绿色合成
Pub Date : 2014-02-13 DOI: 10.1155/2014/358932
B. Basu, Kinkar Biswas, S. Kundu, Debasish Sengupta
On-water hydrothiolation reaction between terminal alkyne and thiol has been probed in the presence of various additives. Aromatic alkynes yield corresponding 1-alkenyl sulfides, whereas aliphatic alkynes undergo double-addition yielding vicinal disulfides in good to excellent yields. Formation of 1-alkenyl sulfides proceeds with a high degree of regioselectivity (via anti-Markovnikov addition), and switching the stereoselectivity between E/Z isomers has been noticeably realized in the presence of different additives/promoters.
在不同添加剂的作用下,探讨了末端炔与硫醇在水中的氢硫化反应。芳香族炔烃生成相应的1-烯基硫化物,而脂肪族炔烃经过两次加成生成邻二硫化物,收率很高。1-烯基硫化物的形成具有高度的区域选择性(通过反马尔可夫尼科夫加成),并且在不同添加剂/促进剂的存在下,E/Z异构体之间的立体选择性转换已经明显实现。
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引用次数: 3
Green Chemistry: New Synthesis of Substituted Chromenes and Benzochromenes via Three-Component Reaction Utilizing Rochelle Salt as Novel Green Catalyst 绿色化学:以罗谢尔盐为新型绿色催化剂的三组份反应新合成取代铬和苯并铬
Pub Date : 2014-01-30 DOI: 10.1155/2014/715091
A. El-Maghraby
Substituted 2-amino-4-aryl-7-hydroxy-4H-chromene-3-carbonitriles (6), 2-amino-4-aryl-4H-benzo[h]chromene-3-carbonitriles (7), and 3-amino-1-aryl-1H-benzo[f]chromenes-2-carbonitriles (8) were prepared, in good yields, via one-pot three-component reactions of aromatic aldehydes (1), malononitrile (2), and resorcinol (3) or α-naphthol (4) or β-naphthol (5) in refluxing ethanol or water in the presence of Rochelle salt as novel green heterogeneous and reusable catalyst.
以芳香醛(1)、丙二腈(2)、间苯二酚(3)或α-萘酚(4)或β-萘酚(5)为催化剂,以Rochelle盐作为新型绿色非均相可重复使用的催化剂,在乙醇或水回流条件下,通过一锅三组分反应,以较好的收率制备了取代的2-氨基-4-芳基-4-羟基-4-铬-3-碳腈(6)、2-氨基-4-芳基-4-苯并[h]铬-3-碳腈(7)和3-氨基-1-芳基-1-苯并[f]铬-2-碳腈(8)。
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引用次数: 18
An Efficient and Green Method for Synthesis of 2,4,5-Triarylimidazoles without Use of Any Solvent, Catalyst, or Solid Surface 一种高效、绿色的合成2,4,5-三芳基咪唑的方法,无需任何溶剂、催化剂或固体表面
Pub Date : 2013-12-10 DOI: 10.1155/2013/512074
Swati Samanta, Saheli Sarkar, R. Pal, A. Mallik
An efficient and green method for synthesis of 2,4,5-triarylimidazoles without use of any catalyst or solvent has been developed simply by heating (at 130°C) of mixtures of 1,2-diketone, aromatic aldehyde, and ammonium acetate in 1 : 1 : 3 mole ratio.
在130℃下,将1,2-二酮、芳香醛和乙酸铵以1:1:3的摩尔比加热合成2,4,5-三芳基咪唑,获得了一种高效、绿色的合成方法。
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引用次数: 4
Synthesis of Pyrazine Substituted 1,3,4-Thiadiazole Derivatives and Their Anticonvulsant Activity 吡嗪取代1,3,4-噻二唑衍生物的合成及其抗惊厥活性
Pub Date : 2013-12-04 DOI: 10.1155/2013/631723
K. Harish, K. Mohana, L. Mallesha
The synthesis of new pyrazine substituted 1,3,4-thiadiazole derivatives was carried out in good yield by the reaction of pyrazine substituted 1,3,4-thiadiazoles with various sulfonyl chlorides. A chemical structure of all the new compounds was confirmed by 1H NMR and mass spectral data. The new compounds were screened for their anticonvulsant activity against maximal electroshock (MES) seizure method. Rotarod method was employed to determine the neurotoxicity. Few compounds showed significant changes in anticonvulsant activity. The same compounds showed no neurotoxicity at the maximum dose administered (100 mg/kg).
以吡嗪取代的1,3,4-噻二唑为原料,与各种磺酰氯反应,合成了新的吡嗪取代的1,3,4-噻二唑衍生物,收率较高。所有新化合物的化学结构都通过1H NMR和质谱数据得到了证实。新化合物对最大电休克(MES)发作法的抗惊厥活性进行了筛选。采用轮棒法测定神经毒性。很少有化合物在抗惊厥活性方面表现出显著的变化。相同的化合物在最大剂量(100 mg/kg)下没有神经毒性。
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引用次数: 9
期刊
Organic Chemistry International
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