Palladium and Copper Cocatalyzed Intermolecular Cyclization Reaction: Synthesis of 5‐Aminopyrazole Derivatives

A novel and efficient palladium and copper co‐catalyzed intermolecular cyclization of acetonitriles with hydrazones has been developed for the synthesis of 5‐aminopyrazoles through C C and C N bond formation. The reaction has the advantages of easily available starting materials, simple manipulation and mild reaction conditions. The reaction involving various substituted acetonitriles and hydrazones proceeds smoothly and 5‐aminopyrazoles are synthesized in good yields. In contrast to the aliphatic and heteroaromatic substrates, the aromatic substrates tend to have a higher degree of reactivity.

     

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.

     

Copper‐Catalyzed Allenylation‐Isomerization Sequence of Penta‐1,4‐diyn‐3‐yl Acetates with P(O)H Compounds: Facile Synthesis of 1‐Phosphonyl 2,4‐Diynes

The copper‐catalyzed reaction of 5‐substituted penta‐1,4‐diyn‐3‐yl acetates with P(O)H compounds to efficiently give a new class of phosphonyl diynes is reported. The reaction may take place through a regioselective nucleophilic attack of phosphorus nucleophiles on Cu‐allenylidene intermediates to form allenyl intermediates followed by a rapid allene‐alkyne isomerization process. The synthetic utility of the obtained products is demonstrated.

     

Constructing porous ZnO/SnO2 nanocomposites for the detection of methane at low operating temperature

Journal of Porous Materials - Aimed at detecting methane (CH4) gas at low operating temperature, porous ZnO/SnO2 nanocomposites were constructed through a simple two-step method. Pure SnO2 with a...     

Synthesis of 3D graphene/MnO2 nanocomposites with hierarchically porous structure for water purification

Journal of Porous Materials - In this work, a three-dimensional (3D) graphene/manganese dioxide nanocomposite (PGA/MnO2) with a hierarchically porous structure was prepared by facile steam...     

聚四氟乙烯未烧结带的分类及应用

介绍了聚四氟乙烯分散树脂及未烧结带的特点,综述了聚四氟乙烯未烧结带的分类和应用,指出了其存在的问题,并对未来的发展进行了展望。     

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.     

拱悬挂结构在大跨体育建筑中的形态表现与应用解析

拱悬挂结构是混合吊挂结构体系中较为常见且极具表现特色的结构形式之一,在大跨体育建筑中多有应用.本文从结构受力及形态的角度出发,分别对拱悬挂结构的特质、应用形态和表现特征进行解析,为更广范意义上结构形态设计指导下的大跨建筑创作提供思路.     

呼和浩特回族聚居区的保护与更新发展

本文以呼和浩特回族聚居区为切入点,分析其特色与保护价值。针对目前城市发展过程中存在的一系列问题,提出统一协调建筑特色、完善人性化设施、大力发展民族特色产业等观点。