Enantioselective Construction of Cyclic Enaminone‐Based 3‐Substituted 3‐Amino‐2‐oxindole Scaffolds via Catalytic Asymmetric Additions of Isatin‐Derived Imines

The first catalytic asymmetric construction of the cyclic enaminone‐based 3‐substituted 3‐amino‐2‐oxindole scaffold with potential bioactivity has been developed via chiral phosphoric acid‐catalyzed enantioselective addition reactions of cyclic enaminones to isatin‐derived imines, which afforded a series of cyclic enaminone‐based 3‐substituted 3‐amino‐2‐oxindoles in high yields and excellent enantioselectivities (up to 99% yield, 97% ee). The investigation of the reaction mechanism suggested that it was facilitated by a dual hydrogen‐bonding activation mode between the two substrates and the chiral phosphoric acid. Besides, this method could be utilized for a large‐scale synthesis with maintained enantioselectivity. This approach will not only offer a useful method for enantioselective construction of the cyclic enaminone‐based 3‐substituted 3‐amino‐2‐oxindole scaffold, but also enrich the research on catalytic asymmetric addition reactions of isatin‐derived imines by using electron‐rich olefins as nucleophiles. More importantly, a preliminary evaluation on the cytotoxicity of some selected products revealed that two of the enantio‐pure compounds exhibited moderate to strong cytotoxicity to A549, 786‐0, ECA109 and BT474 cancer cell lines.

     

Preparation of lightweight and hydrophobic natural biomass-based carbon aerogels for adsorption oils and organic solvents

Journal of Porous Materials - In the present work, an excellent carbon aerogel (PCA) with low density, hydrophobicity and porous structure has been successfully prepared by hydrothermal...     

Tailoring acidity of HZSM-5 nanoparticles for methyl bromide dehydrobromination by Al and Mg incorporation

Three kinds of HZSM-5 nanoparticles with different acidity were tailored by impregnating MgO or varying Si/Al ratios. Both the textural and acidic properties of the as-prepared nanoparticles were characterized by nitrogen adsorption-desorption measurements, X-ray diffraction (XRD), scanning electron microscopy (SEM), ammonia temperature-programmed desorption (NH₃-TPD) and Fourier transform infrared spectroscopy (FTIR or Py-FTIR). It was found that the intensity of Lewis acid sites with weak strength was enhanced by impregnating MgO or reducing Al concentration, and such an enhancement could be explained by the formation of Mg(OH)⁺ or charge unbalance of the MgO framework on the surface of HZSM-5 support. The effect of HZSM-5 nanoparticles'' acidity on methyl bromide dehydrobromination as catalyst was evaluated. As the results, MgHZ-360 catalyst with the highest concentration of Lewis acid sites showed excellent stability, which maintained methyl bromide conversion of up 97% in a period of 400 h on stream. Coke characterization by BET measurements and TGA/DTA and GC/MS analysis revealed that polymethylated naphthalenes species were formed outside the channels of the catalyst with higher acid intensity and higher Brønsted acid concentration during the initial period of reaction, while graphitic carbon formed in the channels of catalyst with lower acid intensity and higher Lewis acid concentration during the stable stage.     

Rapid Carbonation for Calcite from a Solid-Liquid-Gas System with an Imidazolium-Based Ionic Liquid

Aqueous carbonation of Ca(OH)₂ is a complex process that produces calcite with scalenohedral calcite phases and characterized by inadequate carbonate species for effective carbonation due to the poor dissolution of CO₂ in water. Consequently, we report a solid-liquid-gas carbonation system with an ionic liquid (IL), 1-butyl-3-methylimidazolium bromide, in view of enhancing the reaction of CO₂ with Ca(OH)₂. The use of the IL increased the solubility of CO₂ in the aqueous environment and enhanced the transport of the reactive species (Ca²⁺ and CO₃²⁻) and products. The presence of the IL also avoided the formation of the CaCO₃ protective and passivation layer and ensured high carbonation yields, as well as the production of stoichiometric rhombohedral calcite phases in a short time.     

Pharmacokinetic Comparison of Berberine in Rat Plasma after Oral Administration of Berberine Hydrochloride in Normal and Post Inflammation Irritable Bowel Syndrome Rats

In the present study, post inflammation irritable bowel syndrome (PI-IBS) rats were firstly established by intracolonic instillation of acetic acid with restraint stress. Then the pharmacokinetics of berberine in the rat plasma were compared after oral administration of berberine hydrochloride (25 mg/kg) to normal rats and PI-IBS rats. Quantification of berberine in the rat plasma was achieved by using a sensitive and rapid UPLC-MS/MS method. Plasma samples were collected at 15 different points in time and the pharmacokinetic parameters were analyzed by WinNonlin software. Compared with the normal group, area under the plasma concentration vs. time curve from zero to last sampling time (AUC_0–t) and total body clearance (CL/F) in the model group significantly increased or decreased, (2039.49 ± 492.24 vs. 2763.43 ± 203.14; 4999.34 ± 1198.79 vs. 3270.57 ± 58.32) respectively. The results indicated that the pharmacokinetic process of berberine could be altered in PI-IBS pathological conditions.     

血管内皮细胞生长因子C及其受体3在结直肠癌转移中的作用

结直肠癌是最常见胃肠道恶性肿瘤之一,它的转移扩散是其预后不良的常见原因。结直肠癌虽然可通过多种途径进行扩散,但是淋巴管侵袭和淋巴转移是常见的早期事件。血管内皮生长因子-C（VEGF-C）是近年来发现的与结直肠癌密切相关的基因,VEGF-C及血管内皮生长因子受体3（VEGFR-3）在结直肠癌的淋巴管生成和淋巴转移中发挥了重要作用。     

浅谈桥面铺装层裂缝产生的原因与修补措施

近年来,由于高速公路的损坏而导致的交通事故越来越多,所以逐渐引起了人们的重视。水泥混凝土桥面板破损往往是面积最大的、也是最严重的,其他比较常见的病害有桥面铺装层破损、开裂、错台、麻面和磨光等。     

永磁电磁轴承自检测原理

为了降低磁悬浮轴承的制造成本,提高磁悬浮系统的动态性能,提出了自检测磁悬浮轴承系统.该自检测系统从电磁轴承控制线圈两端提取随位移变化的电感电压(电流)信号,作为反馈信号,构成伪微分反馈(PDF)控制的闭环自检测磁悬浮轴承系统.试验结果表明,该自检测磁悬浮轴承系统具有很强的鲁棒性.     

碳纳米管/ZM5复合材料的高温拉伸性能与显微组织

在氩气保护下,采用搅拌铸造法制备了碳纳米管(CNTs)/ZM5镁合金复合材料;测试了铸态下其高温拉伸性能,并对其显微组织和断口形貌进行了分析.结果表明:该复合材料具有良好的高温拉伸性能,在拉伸速率为1mm·min-1以及温度为473K时其抗拉强度可达117.65MPa,比基体提高了20%;当CNTs加入量为0.5%时,其最大伸长率达到8.32%,比基体提高了21.62%;在高温下该复合材料的断裂形貌主要由韧窝和撕裂棱所组成.     

力反馈虚拟手术器械的设计

设计了一种二维虚拟手术器械,提出一种机械结构设计方案,以及软件实施方案.研究了虚拟手术器械设计中一些关键问题,如元器件选择,电机堵转等,并通过实验建立了电机堵转状况下的力矩模型.