Improved synthesis of the thiophenol precursor N-(4-chloro-3-mercaptophenyl)picolinamide for making the mGluR4 PET ligands

Recently [¹¹C]mG4P012 (previously [¹¹C]KALB012 and presently named as [¹¹C]PXT012253 by Prexton Therapeutics) had been used as a biomarker during the preclinical development of a potential therapeutic drug, PXT0002331 (an mGluR4 PAM), for PD and l-dopa-induced dyskinesia. [¹¹C]mG4P012 was shown to be a promising PET radioligand for mGluR4 in the monkey brain and for further development in human subjects. However, the previously reported multi-step synthesis of the thiophenol precursor suffered from low yields and difficult workup procedures. To support the translational research of [¹¹C]mG4P012 and the other potential applications, we have developed a new route for synthesis of the thiophenol precursor and optimized the reaction conditions. The synthesis of N-(4-chloro-3-mercaptophenyl)picolinamide from 1-chloro-4-nitrobenzene has been greatly improved from 8% to 52% total yield with easy handling and in gram scales.     

Electrochemical Behavior of Dental Ni‐Cr Wirolloy Coated with Eco‐friendly Films in Artificial Saliva

The electrochemical corrosion behavior of the non‐precious Ni‐Cr Wirolloy, being used in dentistry, was investigated before and after applying of two types of eco‐friendly coatings, polyvinyl silsesquioxane (PVS) and nano‐hydroxyapatite (nHAP) separately in artificial saliva solution at 37 °C for 14 d of immersion. The study aimed to investigate the effectiveness of the introduced coating films in enhancing the corrosion resistance of the alloy, and in decreasing the leaching of the toxic Ni ions from the alloy into the environment. The electrochemical corrosion investigation methods used are; open circuit potential (OCP), electrochemical impedance spectroscopy (EIS) and potentiodynamic polarization techniques. The evaluated results revealed that the electrochemically coated alloy with PVS. prepared at cathodic potential showed higher corrosion resistance and more stable film compared to that prepared by conventional dip‐coating method. At the same time, the nHAP electrochemically coated film provided the best anti‐corrosion properties over all examined time intervals. The obtained results were confirmed via surface analysis, which assured the formation of the prepared coatings on the alloy surface. Chemical analysis of the corrosion product/solutions showed that the effect of electrochemically deposited nHAP and PVS. polymer films in suppression of Ni ions leaching is similar and slightly higher than that of the chemically coated PVS. one; however, all of them are efficient in decreasing the leaching of the risky Ni ions into the solution.     

反-4-羟甲基哌啶-3-醇的合成

以4-羟甲基吡啶为原料,经苄基保护、硼氢化钠的还原、硼氢化氧化和脱苄基保护等四步反应得到新型5-羟色胺受体激动剂的关键中间体反-4-羟甲基哌啶-3-醇。总收率达55. 7%。产物结构经IR、1H NMR和MS分析确证,并对合成工艺进行了优化。     

Protective Effect of Potentilla glabra in UVB-Induced Photoaging Process

Maintaining skin homeostasis is one of the most important factors for skin health. UVB-induced skin photoaging is a difficult problem that has negative impacts on skin homeostasis. So far, a number of compounds have been discovered that improve human skin barrier function and hydration, and are thought to be effective ways to protect skin homeostasis. Potentilla glabra var. mandshurica (Maxim.) Hand.-Mazz. Ethanol Extract (Pg-EE) is a compound that has noteworthy anti-inflammatory properties. However, its skin-protective effects are poorly understood. Therefore, we evaluated the capacity of Pg-EE to strengthen the skin barrier and improve skin hydration. Pg-EE can enhance the expression of filaggrin (FLG), transglutaminase (TGM)-1, hyaluronic acid synthase (HAS)-1, and HAS-2 in human keratinocytes. Moreover, Pg-EE down-regulated the expression of pro-inflammatory cytokines and up-regulated the production of FLG, HAS-1, and HAS-2 suppressed by UVB through inhibition of p38 mitogen-activated protein kinase (MAPK) and extracellular signal-regulated kinase (ERK) pathways. Given the above, since Pg-EE can improve skin barrier, hydration and reduce the UVB-induced inflammation on skin, it could therefore be a valuable natural ingredient for cosmetics or pharmaceuticals to treat skin disorders.     

电化学应用技术在课堂教学中的渗透

在高职课堂讲授电化学知识时,精心设计教学内容,采用模块教学法,将前沿的电化学应用技术渗透在课堂教学中,针对材料专业学生的电化学教学实施思路,适当简化基础理论,让学生了解电化学在新能源、新材料、环境监测等领域的实用技术。     

在高职药物化学教学中融入绿色化学理念

绿色环保是社会发展的趋势,培养绿色环保的理念和技能是人才教育的责任。药物化学是高职高专药学类专业的核心课程,教学中尝试以绿色化学的12条原则为主线,引入实例,将绿色化学的理念和实施方法运用到药物化学的结构设计和工艺路线中,从而让学生理解绿色化学的12条原则,丰富学生关于药学领域的绿色化学经验和技能。     

水性氧化石墨烯/聚苯胺复合材料制备及其防腐性能研究

采用液相法制备了一种水性氧化石墨烯/聚苯胺复合材料.通过SEM、XRD等手段对复合材料进行了表征,并对制备的复合涂层进行电化学分析和理化性能测试.结果表明,在有机酸的存在下,苯胺单体以充分剥离的氧化石墨烯为成核生长位点,形成了分散良好的氧化石墨烯/聚苯胺复合材料,并保持了氧化石墨烯的层状结构.在复合涂层中,掺杂在聚苯胺分子骨架上的磺基水杨酸(SSA)或十二烷基苯磺酸(DBSA)与聚苯胺协同形成电化学保护作用,有效地将2A12铝合金的腐蚀电流最低降至2×10-7A/cm2左右.该涂层具有良好的强度、韧性和附着等力学性能,并且具有优良的耐盐雾、光照老化等物理稳定性.     

表面硅烷化铜箔的电化学腐蚀与防护研究

用γ-氨丙基三甲氧基硅烷(γ-APS)溶液对铜箔表面硅烷化处理,采用动电位极化和电化学交流阻抗研究不同pH的γ-氨丙基三甲氧基硅烷溶液自组装铜箔电极在0.1 mol.L^-1NaCl溶液的腐蚀防护效果,采用扫描电子显微镜观察γ-氨丙基三甲氧基硅烷自组装膜的表面形貌.结果表明,γ-氨丙基三甲氧基硅烷自组装铜箔有较好的腐蚀防护效果,其中pH=7的γ-氨丙基三甲氧基硅烷溶液自组装膜的抗腐蚀效果最佳.     

轻质多层热防护结构的一体化优化设计研究

大面积防热结构在航天航空领域应用广泛, 其创新结构设计是关键技术之一. 航天飞行器的工作条件要求热防护材料与结构同时具备轻质、隔热、抗冲击的特点, 因此热防护材料与结构正在朝着一体化的方向发展. 基于这种发展趋势, 提出了一种轻质多层热防护结构设计方案. 以一体化多层防热结构在航天器再入过程中的传热为研究对象, 引入大面积防热结构的一维传热假设, 依照航天器再入大气层的温度条件, 建立了防热结构一维非稳态传热的物理模型和封闭的控制方程, 使用差分方法求解方程, 进行一维非稳态的传热分析, 并采用商业有限元软件ABAQUS的传热分析进行验证. 得到了航天器再入大气过程中多层防热结构的各层温度分布, 提出了在满足一定的热约束要求的条件下, 以轻质多层热防护结构的总重量为目标函数的优化设计方法, 得到了多层结构的最优几何参数, 并将优化后的结构进行了有限元承载分析.      

Ti/IrO_2-Ta_2O_5阳极载量与析氧电催化性能研究

采用Pechini法制得Ti/IrO2-Ta2O5氧化物阳极,研究了涂层载量对Ti/IrO2-Ta2O5阳极微观结构和析氧电催化性能的影响.SEM、EDX、极化曲线、循环伏安及强化电解试验等测试结果表明:涂层载量增加,涂层裂缝变窄变浅,且IrO2晶粒偏析趋于增强;同时也提高了阳极析氧电催化活性,增大阳极活性表面积及延长阳极使用寿命;强化电解寿命与Ir涂覆量(1.98～9.08g/m2)基本呈线性递增关系.