烯丙基酚类衍生物的简便合成

烯丙基酚类衍生物的简便合成;相转移催化;Claisen重排;甲基二烯丙基苯酚     

皂甙类化合物解簇集行为的研究

用荧光光谱方法研究了筇甙类化合物在Φ=0.60 DX-H_2O溶液中对探针Np-8- Ch簇集体的解簇集行为，讨论了皂甙类化合物结构与解族集能力间的关系。并结合 细胞粘附实验，探讨了此类化合物解簇集能力与它们药物功能之间的联系。     

N－丙烯酰基－N＇－苯基脲及其衍生物的合成与聚合反应

 以三种合成路线分别合成了含有脲键的一类单体，Ｎ－丙烯酰基－Ｎ’－苯基脲（ＡＰＵ）、Ｎ－甲基丙烯酰基－Ｎ’－苯基脲（ＭＰＵ）、Ｎ－甲基丙．烯酰基－Ｎ’－对甲苯基脲（ＭＴＵ），通过单体的自由基聚合与共聚合，制备了均聚物和共聚物，经ＩＲ、１Ｈ—ＮＭＲ表征和ＴＧＡ、ＤＳＣ测定．     

氟烷基取代的双酚A类衍生物的合成

利用相转移催化剂十六烷基三甲基溴化铵(CTMAB)催化的连二亚硫酸钠引发的苯酚衍生物与含氟碘代烷的氟烷基化反应, 合成了含氟烷基取代的酚类化合物. 研究了双酚A与含氟碘代烷的氟烷基化反应, 得到了一类重要的含氟单体, 即含氟烷基取代的双酚A衍生物. 通过改变含氟碘代烷与双酚A的摩尔比, 可以得到单取代、二取代和四取代的含氟烷基双酚A衍生物.     

四种苯酚衍生物在水溶液中扩散系数的QSAR研究

以Winmopac7软件中AM1量子化学半经验分子轨道方法计算苯酚、邻苯二酚、间苯二酚、对苯二酚和邻苯三酚的水合物的结构参数,利用多元线性回归方法研究了以上5种酚的扩散系数与其分子结构参数之间的关系.结果表明,4种苯酚衍生物的扩散系数与分子的电子能量(Ee),分子的总偶极矩(μT),分子的体积(Vm)有较好的相关性.其回归方程为DT=1.155×10-5+3.675×109 Ee+4.734×10-7μT-9.28×10-3 Vm,R2=0.999 2 SD=1.428×10-7利用此方程预测邻苯三酚的扩散系数为(2.045±0.143)×10-6 cm2/s.此结果表明,AM1量子化学半经验分子轨道方法在对酚类化合物的扩散系数的研究和预测上具有可适用性,此方法也为其他有机化合物在水溶液中的扩散系数的研究和预测提供了新思路和新方法.     

苯胺及其衍生物的毛细管电泳行为研究

采用紫外吸收检测，毛细管电泳分离，研究了九种苯胺及其衍生物在毛细管区带电泳(CZE)体系和胶束电动毛细管色谱(MECC)体系中的行为特征。讨论了缓冲溶液的浓度与pH、胶束浓度及混合胶束等在不同体系中对分离组分的影响，发现在CZE体系中，控制分离的主要因素是pKb值；在MECC体系中，控制分离的主要因素是溶质分子中碳原子数。建立了一种分离测定九种苯胺及其衍生物的高效毛细管电泳方法。     

2—芳基苯并恶唑衍生物与物理行为研究

对２－芳基苯并恶唑衍生物的光谱及光物理行为进行了研究。结果表明，该系列化合物与常见分子内共轭电荷转移化合物的特性明显不同。分析了存在差异的原因，指出该类化合物的较强的荧光发射能力与其分子中的Ｃ＝Ｎ双键的异构化受阻密切相关。     

D301树脂对酚类的吸附热力学研究

测定D301树脂对环己烷溶液中苯酚的吸附等温线，利用热力学函数关系计算了等量吸附焓，吸附自由能和吸附熵，等量吸附焓在30kJ/mol-35kJ/mol之间，推测吸附过程为氢键吸附。比较D301树脂对水溶液和环己烷溶液中苯酚的吸附性能，及D301树脂对环己烷溶液中苯酚和邻硝苯酚的吸附性能，进一步讨论了D301树脂对酚类物质吸附中的氢键作用。     

抗癌药物喜树碱衍生物的研究

喜树碱是一种天然抗癌药物,通过对喜树碱20位羟基的修饰和对喜树碱E环扩环,来提高该类化合物的活性并减小毒性,起到更好的治疗效果。简单介绍喜树碱衍生物的研究现状及其未来的发展趋势。     

酰肼衍生物的凝胶化行为

N,N-(5-烷氧基-1,3-苯二甲酰)-N',N'-二(4-甲基苯甲酰)二肼系列化合物(An)能在苯、甲苯、硝基苯及氯仿等有机溶液中形成有机凝胶. X射线衍射实验及扫描电子显微镜观察的结果显示, 在凝胶状态下, An分子聚集成层状有序排列, 并进一步堆积形成纤维网络结构. 红外光谱及核磁氢谱研究证实了分子间氢键码酰肼衍生物形成凝胶的驱动力. 另外, 侧链上烷基链的长度对凝胶的能力及凝胶的稳定性影响较大, 而对于凝胶的形貌及分子聚集的结构影响不大.     

Study on the Aggregation and Deaggregation Behaviors of Phosphatidylcholines

Phosphatdylcholines and their analogs, the functional building block of the membrane, are recently found to mediate multiple physiological processes and exhibit a broad range of desirable pharmacological effects, which involve hydrophobic lipophilic interactions (HLI) between the phospholipid and the cell membrane. The HLI behavior of phosphatJdylcholines (Ln) and their analogues 1, 2-diacyl-sn-glycerol-3-phosphoric acid bromoethyl ester (Pn), have been investigated in MeOH-H20 binary systems of different volume fractions (designated as Φ) of the organic component, by employing α-nephthylethyl lauryl ether (Np-12) as fluorescent probe. A very interesting observation is that the Ln possesses double character, i. e., it behaves both as an aggregator and as a deaggregator. The effects of the structure and the environment on the coaggregation and deaggregtion are also discussed.     

不同4-氨基吡唑啉酮衍生物在在线富集和测定总酚中的应用

本文合成了几种4-氨基吡唑啉酮衍生物,比较了它们在铁氰化钾存在下与苯酚及其衍生物的反应,并利用这些反应生成的化合物于自行设计的流动注射分析系统,实现了总酚在线分离富集。讨论了不同氨基吡唑啉酮衍生物对在线分离富集的影响。测定总酚的灵敏度可达μg／L级,比常规的光度方法提高了2个数量级。而且本方法简便可行、重现性好。     

Fluorescent Recognition of Small Organic Molecules Based on Supramolecular Aggregation/Deaggregation of Planar Cu(II) Coordination Complex

A Cu(II) coordination complex ( 1 ) with Schiff ligand derived from diaminomaleonitrile was synthesized and characterized, in which the ligand is rigid, planar and conjugated. The complex 1 displays an interesting fluorescent property relative to solvents which can be turned‐on by CH₂Cl₂ and CHCl₃ solvent molecules. The mechanism of this selective fluorescence emission has been studied based on the crystal structure and the spectrum analysis. The tuning on and off fluorescence of complex 1 can be controlled by the process of supramolecular aggregation/deaggregation in different solvents.     

Polycyclic Phenol Derivatives from the Leaves of Spermacoce latifolia and Their Antibacterial and α-Glucosidase Inhibitory Activity

Three new polycyclic phenol derivatives, 2-acetyl-4-hydroxy-6H-furo [2,3-g]chromen-6-one (1), 2-(1′,2′-dihydroxypropan-2′-yl)-4-hydroxy-6H-furo [2,3-g][1]benzopyran-6-one (2) and 3,8,10-trihydroxy-4,9-dimethoxy-6H-benzo[c]chromen-6-one (8), along with seven known ones (3–7, 9 and 10) were isolated for the first time from the leaves of Spermacoce latifolia. Their structures were determined by spectroscopic analysis and comparison with literature-reported data. These compounds were tested for their in vitro antibacterial activity against four Gram-(+) bacteria: Staphyloccocus aureus (SA), methicillin-resistant Staphylococcus aureus (MRSA), Bacillus cereus (BC), Bacillus subtilis (BS), and the Gram-(−) bacterium Escherichia coli. Compounds 1, 2, 5 and 8 showed antibacterial activity toward SA, BC and BS with MIC values ranging from 7.8 to 62.5 µg/mL, but they were inactive to MRSA. Compound 4 not only showed the best antibacterial activity against SA, BC and BS, but it further displayed significant antibacterial activity against MRSA (MIC 1.95 µg/mL) even stronger than vancomycin (MIC 3.9 µg/mL). No compounds showed inhibitory activity toward E. coli. Further bioassay indicated that compounds 1, 4, 5, 6, 8 and 9 showed in vitro α-glucosidase inhibitory activity, among which compound 9 displayed the best α-glucosidase inhibitory activity with IC₅₀ value (0.026 mM) about 15-fold stronger than the reference compound acarbose (IC₅₀ 0.408 mM). These results suggested that compounds 4, 8 and 9 were potentially highly valuable compounds worthy of consideration to be further developed as an effective anti-MRSA agent or effective α-glucosidase inhibitors, respectively. In addition, the obtained data also supported that S. latifolia was rich in structurally diverse bioactive compounds worthy of further investigation, at least in searching for potential antibiotics and α-glucosidase inhibitors.     

水相中取代苯酚的硫酸氢钠/硝酸钠硝化反应

以硫酸氢钠和硝酸钠为硝化剂,在水溶液中完成了取代苯酚的硝化反应.硝化产物具有良好的选择性和较高的产率.     

1,4-二氢吡啶衍生物的电化学行为

1;4-二氢吡啶衍生物的电化学行为;循环伏安法     

新型噻吩并四氢吡啶类化合物的合成及其抗血小板聚集活性

噻吩并［3,2-c］四氢吡啶和噻吩并［2,3-c］四氢吡啶分别与取代苄溴(2a~2g)经取代反应后,用2 mol·L^-1氯化氢乙醚溶液成盐合成了噻吩并四氢吡啶衍生物(3b~3e, 3g和5a~5g);噻吩并［3,2-c］四氢吡啶酮与取代苄溴经取代反应,再与乙酸酐缩合,最后经2 mol·L^-1氯化氢乙醚溶液成盐合成了噻吩并四氢吡啶衍生物(7d, 7e, 7g~7i)。 3, 5和7均为新化合物,其结构经¹H NMR 和ESI-MS表征。大鼠体内抗血小板聚集活性研究结果表明：3, 5和7均有一定的抗血小板聚集活性,其中7d, 7h和7i的抑制率分别为66.2%, 86.8%和88.3%,活性优于阳性对照药噻氯匹啶。