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2,3-二氢喹唑啉-4(1H)-酮是一类重要的含氮稠杂环化合物,具有广泛的药理及生物活性,在药物合成与研发领域有着重要应用价值,因而其合成方法也倍受人们关注.归纳总结了2,3-二氢喹唑啉-4(1H)-酮类化合物的合成研究进展,主要介绍了以邻氨基苯甲酰胺、靛红酸酐、邻硝基苯甲酰胺、邻叠氮基苯甲酰胺、邻溴苯甲酰胺、邻溴苯甲腈、邻氨基苯甲酸、邻氨基苯甲腈、邻氨基N-甲基-N-丙二烯基苯甲酰胺、N-烷基苯胺等为起始原料的2,3-二氢喹唑啉-4(1H)-酮类化合物的合成研究进展概况及其反应机理.最后对该类化合物的合成研究进展进行了总结,并对其发展前景进行了展望. 相似文献
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设计合成了一系列2,3-二取代喹唑啉-4(3H)-酮化合物,并研究了常用无机干燥剂对目标化合物合成的影响,发现无水硫酸镁能够促进2,3-二取代喹唑啉-4(3H)-酮化合物的形成.所有化合物通过核磁共振氢谱、核磁共振碳谱、高分辨质谱等方法进行结构表征,并首次报道了6-氯-3-苄氨基-2-新戊基-8-甲基喹唑啉-4(3H)-酮的单晶结构.通过生物活性测试发现部分化合物在200 mg/L浓度下对小麦白粉病(Blumeria graminis)具有较好的活体防效. 相似文献
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在NaHSO4催化下,以苯甲醛和邻氨基苯甲酰胺为底物,在室温下合成了一系列2-芳基-2,3-二氢-4(1H)-喹唑啉酮类化合物,该反应产率高、操作简单、并且避免使用有毒的金属催化剂. 相似文献
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为进一步发现提高氟喹诺酮抗肿瘤活性的有效结构修饰策略,基于片段药物设计原理,通过喹啉-4(1H)-酮与芳香醛缩合反应合成了(S)-6-氟-7-(4-甲基-哌嗪-基)-8,1-(1,3-氧丙基)-3-芳苄叉基-2,3-二氢-喹啉-4(1H)-酮(3a-3l)目标化合物。 体外抗肿瘤活性结果表明,所合成的12个新化合物的活性均强于母体左氧氟沙星,其中F、Cl、Br取代的卤苯基化合物对人肝癌细胞株(SMMC-7721)和人胰腺癌细胞株(Capan-1)的半数抑制浓度(IC50)低于其它取代基化合物,尤其是氯苯基化合物(3k)与对照抗肿瘤药阿霉素活性相当。 为此,芳苄叉基替代C-3羧基构建的3-芳苄叉基-喹啉-4-酮化合物有助于提高氟喹诺酮的抗肿瘤活性,提示α,β-不饱和酮片段作为一个有发展前景的氟喹诺酮的候选修饰基团值得进一步发展。 相似文献
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《有机化学》2019,(9)
设计合成了3类C(3)-1,2,4-三氮唑取代的1,5-苯并硫氮杂■化合物,2,3-二氢/2,5-二氢/2,3,4,5-四氢-3-(1,2,4-三氮唑)-4-芳基-1,5-苯并硫氮杂■.研究了中间体及目标产物的合成条件,确定了其中2个副产物的结构.目标产物的抑菌活性测试表明,2,3-二氢/2,5-二氢-3-(1,2,4-三氮唑)-4-芳基-1,5-苯并硫氮杂■对新生隐球菌和白色念珠菌表现出很高的抑制作用,在200μg/disc的浓度下,有4个化合物对新生隐球菌的抑制作用高于对照药物氟康唑,有3个化合物对白色念珠菌的抑制活性高于对照药物氟康唑.初步抑真菌构效关系研究表明,1,2,4-三氮唑环和C=N双键是2,3-二氢-3-(1,2,4-三氮唑)-4-芳基-1,5-苯并硫氮杂■抑真菌活性的关键药效团. 相似文献
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采用顺序一锅法,以4,5,7-三氢-吡喃并[4,3-d]噻吩基三苯基膦亚胺、芳基异氰酸酯和胺类化合物为原料,合成了19个结构新颖的5,6,8-三氢吡喃并[3′,4′:4,5]噻吩并[2,3-d]嘧啶-4(3H)-酮衍生物.该方法具有条件温和、操作简便、收率高等特点.所得化合物的结构用1H NMR,IR和MS等手段进行了表征,此外还通过X射线单晶衍射分析法进一步确证了化合物3-(4-氯苯基)-2-二乙胺基-5,6,8-三氢-吡喃并[3′,4′:4,5]噻吩并[2,3-d]嘧啶-4(3H)-酮(4a)的结构. 相似文献
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MIAO Ru XU ZhenXiang HUANG ZhiTang & CHEN ChuanFeng Beijing National Laboratory for Molecular Science 《中国科学B辑(英文版)》2009,52(4):505-512
A series of novel N,O-type chiral ligands derived from enantiopure inherently chiral calix[4]arenes containing quinolin-2-yl-methanol moiety in
the cone or partial-cone conformation have been synthesized and characterized. Moreover, they have been applied to the catalytic
asymmetric addition of diethylzinc to benzaldehyde, which represents the first example that the inherently chiral calixarene
can be used as the chiral ligands for the catalytic asymmetric synthesis.
Supported by the National Natural Science Foundation of China (Grant Nos. 20625206 & 20372064), the National Basic Research
Project (Grant Nos. 2007CB808000 & 2008CB617501), and the Chinese Academy of Sciences 相似文献
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LanYong Zhang Ying Wan Jiong Zhang Di Li LiHua Wang ShiPing Song ChunHai Fan 《中国科学B辑(英文版)》2009,52(6):746-750
A highly sensitive method for the detection of a breast cancer-associated BRCA-1 gene is reported. The detection is based
on a classical sandwich-type assay using horseradish peroxidase (HRP) as a catalytic label and electrodeposited Os2+/3+ conducting polymer (PAA-PVI-Os) as a redox mediator. Target DNA could be detected by the HRP-catalyzed reduction of H2O2, leading to a limit of detection as low as 10 fM.
Supported by the National Natural Science Foundation of China (Grant Nos. 20725516, 20704043, 20873175 & 20805055), Shanghai
Municipal Commission for Science and Technology (Grant Nos. 0752nm021 & 07ZR14136), Ministry of Science and Technology (Grant
Nos. 2006CB933000, 2007CB936000 & 2007AA06A406), Ministry of Health (Grant No. 2009ZX10603), and China Postdoctoral Science
Foundation and Shanghai Postdoctoral Scientific Program (Grant No. 07R214160). 相似文献
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Field-effect transistor chemical sensors of single nanoribbon of copper phthalocyanine 总被引:1,自引:0,他引:1
Copper phthalocyanine (CuPc) nanoribbon field-effect transistors were implemented as chemical sensors. They showed fast response
and high reversibility in the detection of the tetrahydrofuran atmosphere at room temperature. The drain current of the field-effect
transistor sensor decreased from 6.7 to 0.2 nA when the transistor was measured under the tetrahydrofuran atmosphere. The
sensor was self-refreshable in a few minutes. These results demonstrate that the organic single crystalline nanoribbon transistors
could effectively act as chemical sensors.
Supported by the National Natural Science Foundation of China (Grant Nos. 20721061, 50725311, 60736004, 60771031), the Ministry
of Science and Technology of China (Grant Nos. 2006CB806200, 2006CB932100), and Chinese Academy of Sciences 相似文献
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The equation of the state of the hydrogen bonding fluid system of AaDd type is studied by the principle of statistical mechanics. The influences of hydrogen bonds on the equation of state of the
system are obtained based on the change in volume due to hydrogen bonds. Moreover, the number density fluctuations of both
molecules and hydrogen bonds as well as their spatial correlation property are investigated. Furthermore, an equation describing
relation between the number density correlation function of “molecules-hydrogen bonds” and that of molecules and hydrogen
bonds is derived. As application, taking the van der Waals hydrogen bonding fluid as an example, we considered the effect
of hydrogen bonds on its relevant statistical properties.
Supported by the National Natural Science Foundation of China (Grant Nos. 20303006 and 20574016), the Natural Science Foundation
of Hebei Province (Grant Nos. B2006000959 and B2004000093) and the Natural Science Foundation of Education Committee of Hebei
Province (Grant No. 2003101) 相似文献
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Making use of the invariant property of the equilibrium size distribution of the hydrogen bonding clusters formed in hydrogen
bonding system of AaDd type, the analytical expressions of the free energy in pregel and postgel regimes are obtained. Then the gel free energy
and the scaling behavior of the number of hydrogen bonds in gel phase near the critical point are investigated to give the
corresponding scaling exponents and scaling law. Meanwhile, some properties of intermolecular and intramolecular hydrogen
bonds in the system, sol and gel phases are discussed. As a result, the explicit relationship between the number of intramolecular
hydrogen bonds and hydrogen bonding degree is obtained.
Supported by the National Natural Science Foundation of China (Grant Nos. 20303006 and 20574016), the Natural Science Foundation
of Hebei Province (Grant Nos. B2006000959 and B2004000093) and the Natural Science Foundation of Education Committee of Hebei
Province (Grant No. 2003101) 相似文献
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The water-soluble Ag nanoparticles capped with novel zwitterionic thioalkylated phosphorylcholine were synthesized. The Ag
nanoparticles showed remarkable stability in saline media with salt concentrations as high as 2.0 mol/L and plasma using UV-vis
absorption spectroscopy. Similarly, compared with tiopronin and citrate-protected Ag nanoparticles, the zwitterionic phosphorylcholine
Ag nanoparticles did not precipitate out of solution when charged polyelectrolytes or biopolymers were added. The zwitterionic
phosphorylcholine might be a better ligand for stabilizing metal nanoparticles.
Supported by the National Natural Science Foundation of China (Grant Nos. 20774082 and 50703036), National High Technology
Research and Development Program of China (Grant Nos. 2006AA03Z329 and 2006AA032444) and Science and Technology Projects of
Zhejiang Province (Grant No. 2007C24G2010020) 相似文献
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CoFe2O4/TiO2 magnetic composite films were prepared using the sol-gel method with tetrabutyltitanate and metallic chlorates as starting
materials. The effects of heat treatment temperatures on microstructures and on magnetic properties were studied. The microstructure
and properties of the samples at different heat treatment temperatures were characterized by X-ray diffraction, Raman spectrum,
scanning electron microscopy, polarized microscopy and vibrating sample magnetometry. The results show that crystals of different
substances grow up independently. Cobalt ferrite is evenly embedded into the titanium dioxide matrix in the prepared composite
films. The magnetism of the composite films is enhanced with an increase of the heat temperature.
Supported by the National Natural Science Foundation of China (Grant Nos. 50632030 and 10474077), and the Natural Science
Foundation of Shaanxi Province (Grant No. 2006E135) 相似文献
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Imine-bridged TTF-π-pyridine derivatives, 2NTTF, 3NTTF and 4NTTF, were synthesized and the cation-binding study was performed.
It is noted that with the addition of the micromolar concentration of Pb2+ to the solution, these compounds display remarkable changes in solution color, 1H NMR spectra and electrochemical properties. The nitrogen atom of the imine-bridge in 2NTTF not only serves as a π-conjugated
spacer but also participates in the sensing and coordinating properties.
Supported by the National Natural Science Foundation of China (Grant Nos. 20732007, 20728506 & 20672122), the Ministry of
Science and Technology of China (Grant Nos. 2006CB806105, 2007CB808004, 2007CB936001 & 2009CB-22008) and the Bureau for Basic
Research of the Chinese Academy of Sciences 相似文献
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Using umbrella sampling technique with molecular dynamics simulation, we investigated the nanofluidic transport of water in
carbon nanotube (CNT). The simulations showed that a positive charge modification to the carbon nanotube can slow down the
water column growth process, while the negative charge modification to the carbon nanotube will, on the other hand, quicken
the water column growth process. The free energy curves were obtained through the statistical process of water column growth
under different charge distributions, and the results indicated that these free energy curves can be employed to explain the
dynamical process of water column growth in the nanosized channels.
Supported by the National Natural Science Foundation of China (Grant Nos. 10425420 and 20773145), the Ministry of Science
and Technology of China (Grant Nos. 2006CB806200 and 2006CB932100), and the Chinese Academy of Sciences including its CNIC
Supercomputer Center. 相似文献
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A novel and green method for the synthesis of dimethyl pyridine-3,5-dicarboxylate has been developed. It is PdCl2-catalyzed heterocyclotrimerization of methyl acrylate with urea in methanol/supercritical carbon dioxide. The target compound
was obtained with a 75% isolated yield under the optimized conditions.
Supported by the National Natural Science Foundation of China (Grant Nos. 20332030, 20572027, 20625205 and 20772034) and Guangdong
Natural Science Foundation (Grant No. 07118070) 相似文献