Dearomatization of Indole Derivatives via Palladium‐Catalyzed C?H Bond Functionalization of Pyrroles: Convenient Construction of Spiroindolenines

An intramolecular palladium(II)‐catalyzed dearomative arylation reaction of indoles via C H bond functionalization was developed, providing access to structurally novel spiroindolenines with moderate to good yields. A one‐pot process for the synthesis of spiroindoline derivatives was also realized.

     

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.     

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。     

自行式高空作业平台工业设计研究

以北京京城重工机械有限责任公司产品GTBZ系列高空作业车的转动平台外观造型设计为例,说明了应用计算机辅助工业设计技术,实现高空作业车外观造型设计的设计程序以及其关键技术与方法,阐述了产品结构设计与外形设计同步进行的并行设计思想,并且说明了在计算机三维环境中实现产品的模拟真实感表现的相关内容,根据产品形象设计原理及产品外观的语意学规律,完成了高空作业车的转动平台外观设计和整车的色彩设计。     

压缩垃圾车结构的载荷描述与优化设计

通过建立垃圾堆曲面函数,给出自重、惯性、压缩、挤入和推出等基本工况下压缩垃圾载荷作用机理的变参数数学描述以及各种实际组合工况下压缩垃圾载荷的数学表达式.利用ANSYS软件对压缩垃圾车进行结构有限元分析,调校载荷数学表达中的可变参数,保证分析计算与试验测试结果一致,采用导重法对压缩垃圾车结构的外形与构件尺寸进行优化设计,在结构最大应力从504 MPa下降到176 MPa的同时,结构质量减少29.3 %.     

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.