Fluorine‐18 Radiolabeling and Radiopharmacological Characterization of a Benzodioxolylpyrimidine‐based Radiotracer Targeting the Receptor Tyrosine Kinase EphB4

Members of the Eph receptor tyrosine kinase family play essential roles in the pathogenesis of cancer and are therefore promising candidates for molecular imaging by positron emission tomography (PET), for example. In this regard, radiochemical access to novel PET radiotracers derived from potent inhibitors that target the EphB4 kinase domain and which bear a benzodioxolylpyrimidine structural motif was developed. A synthetic route was established for a new fluorine‐18‐containing radiotracer and for the desired precursor based on a high‐affinity benzodioxolylpyrimidine receptor tyrosine kinase inhibitor lead structure. The radiotracer [¹⁸F] 15 was obtained in 16 % radiochemical yield with a specific activity of ～7 GBq μmol^?1 and >95 % radiochemical purity. Due to the implication of EphB4, particularly in the progression, angiogenesis, and metastasis of melanoma, EphB4‐overexpressing human melanoma cells were generated and used as a novel in vitro model for radiopharmacological evaluation of the radiotracer. We demonstrate that the corresponding non‐radioactive reference compound regained its functionality as an inhibitor for both EphB4 receptor tyrosine kinase and Src kinase. EphB4 was significantly inhibited at compound concentrations >1 μM . Cellular uptake studies with [¹⁸F] 15 revealed substantial uptake in both EphB4‐overexpressing and control cells. Moreover, NMRI nu/nu mice bearing both EphB4‐overexpressing tumors and control tumors were used for radiopharmacological characterization by biodistribution studies ex vivo and by dynamic small‐animal PET experiments in vivo. Despite the high metabolic stability of the novel radiotracer observed in vivo, no substantial binding or accumulation in EphB4‐overexpressing and control tumors was observed. Nevertheless, we point out that the approach presented herein gives convenient access to novel ¹⁸F‐labeled benzodioxolylpyrimidines and is a promising strategy for the further development of novel radiotracers for imaging Eph receptor tyrosine kinases in cancer.     

Tuning the optical bandgap of multi-walled carbon nanotube-modified zinc silicate glass-ceramic composites

Novel glass-ceramic composites with optical bandgap tunability were synthesised. Zinc silicate powder (ZS) was mixed with multi-walled carbon nanotubes (MWCNTs) at various mass fractions (0, 1, 2, and 3 wt %), followed by argon sintering. X-ray diffraction (XRD) analysis revealed the structural change from an amorphous ZS phase to a crystalline willemite phase (Zn₂SiO₄) by adding MWCNTs, and the largest crystallite size was obtained for ZS with 2.0 wt% MWCNTs. Although the agglomeration of ZS and MWCNTs was observed by field emission scanning electron microscopy (FESEM), there was no chemical interaction between ZS and MWCNTs as confirmed by Fourier transform infrared spectroscopy (FTIR). MWCNTs enhanced the crystallisation, which led to the green emission of Zn₂SiO₄ blue-shifting from 572 nm to 557 nm. The narrowed optical bandgap of Zn₂SiO₄ was attributed to the MWCNT-induced exciton localised between the valence band and conduction band of Zn₂SiO₄. The bandgap tuning effect of MWCNTs potentially paved new ways to mass fabricate zinc silicate-based semiconductors with desirable optical bandgap energy E_g, which significantly benefits the sensor and laser-related industry.     

1-戊基-3-甲基咪唑类离子液体的合成

以1-氯戊烷和N-甲基咪唑为原料合成了室温离子液体1-戊基-3-甲基咪唑四氟硼酸盐(PMIMBF4)和六氟磷酸盐(PMIMPF6),通过考察各种影响因素对中间产物氯代咪唑盐(PMIMCl)的影响得出合成1-戊基3-甲基咪唑离子液体的最佳条件为:原料N-甲基咪唑与1-氯戊烷的投料比为1.2∶1,反应温度为70-75℃,反应时间为24 h。最终产物的收率为92%-94%。产物结构用FT-IR和1HNMR光谱进行表征。     

Self-templated nitrogen-doped mesoporous carbon decorated with double transition-metal active sites for enhanced oxygen electrode catalysis

The development of high-performance,low-cost bifunctional catalysts with long-term stability for the oxygen reduction reaction(ORR)and oxygen evolution reaction(OER)is one of the most critical challenges for the large-scale application of metal–air batteries.Herein,we report an advanced nitrogen-doped mesoporous carbon(NMC)composite(NiCo₂O₄/CoN_x–NMC)formed from a mixture of Co-and Ni-hydroxide-infiltrated phenolic resin and melamine resin.This composite exhibits ...     

两种尾式卟啉及其金属钯配合物的合成与表征

合成了尾式卟啉化合物5-(2-戊烷氧基苯基)-10,15,20-三(对氯苯基)卟啉和5-(2-异戊氧基苯基)-10,15,20-三(对氯苯基)卟啉及其金属钯配合物并通过元素分析、紫外-可见光谱、红外光谱和核磁共振氢谱对这些卟啉化合物的结构进行了表征。     

铈离子引发纤维素接枝甲基丙烯酸丁酯制备吸油材料的制备

以棉浆粕为基材,硝酸铈铵/HNO3为引发剂,甲基丙烯酸丁酯(BMA)为接枝单体,N ,N'-亚甲基双丙烯酰胺为交联剂,采用悬浮震荡接枝聚合反应制备了纤维素基吸油材料。采用红外光谱、X射线衍射、扫描电镜、热重分析、差示量热等手段对产物结构进行了表征,考察了棉浆粕的引发及其后的接枝聚合反应,得到最佳工艺条件为：采用含有铈离子的0.15 mol/L的HNO3水溶液在45 ℃下将棉浆粕活化处理2.5 h后,在HNO3水溶液及交联剂存在下,与BMA发生接枝聚合反应;反应配比为纤维素/引发剂/单体/交联剂=1/0.03/1.5/0.03,聚合反应温度为50 ℃,反应时间为24 h。所得纤维素与BMA的接枝共聚物有较高的接枝率及理想的吸油性能。     

准东露天煤矿土壤重金属的污染及空间分布特征分析

本文选择准东露天煤矿为研究区,对煤矿周围111个点进行了土壤样品的采集以及室内试验分析,采用了多元统计分析方法、地累积指数法、潜在生态风险指数法及GIS插值方法分别对Zn、Cu、Cr、Hg、As和Pb六种重金属元素在土壤中的含量,污染状况和空间分布特征进行了统计与插值分析。结果表明:土壤中重金属含量高低顺序为CrZnAsCuPbHg,从重金属含量平均值来看Cr、As和Hg含量分别超过了新疆背景值的1.3倍、13.0倍和3.1倍,国家二级标准值的1.0倍、4.0倍和3.0倍。土壤中Hg的变异系数较大,煤炭开采活动对Hg的影响比较明显。从相关性来看0.01水平上Zn和Cu,Cr和Pb呈线性正相关,相关系数为0.65、0.36,Zn和Cu被认为来自于土壤母质,Cr和Pb被认为主要来自于人为因子,Hg也是主要来自人为因子,As是来自于自然因子和人为因子。污染指数评价结果表明土壤Hg和As含量分别为重度和中度污染,而Zn、Cu、Cr、Pb含量比较低。生态风险评价结果表明了Cr、Zn、As、Cu和Pb处于低风险,Hg处于极重的生态风险。从重金属含量的空间分布情况来看煤田、工业区、生活区及周围地区、卡拉麦里山的南部和靠近沙漠地带土壤重金属含量比较高。     

纤维素氨基甲酸酯纤维纺丝工艺探讨

通过研究纤维素氨基甲酸酯（CC）溶液中CC与NaOH配比（质量比）、溶液纺前处理时间及温度、纺丝凝固浴及再生浴的组成和温度对纤维素氨基甲酸酯溶液可纺性及其纤维性能的影响,得到湿纺工艺制备纤维素氨基甲酸酯纤维的最佳纺丝工艺条件.结果表明：配制CC质量分数为7%,CC与NaOH质量比为1的纤维素氨基甲酸酯的氢氧化钠溶液,在15℃以下进行纺前处理10～12h,溶液可纺性良好．这种溶液在温度为40℃的含H₂SO₄（150g/L）、Na₂SO₄（200g/L）、AI₂（SO₄）₃（50g/L）的凝固浴中成形后,在温度为85℃、质量分数为1%的氢氧化钠水溶液中再生,可得到具有一定强度及伸长率的再生纤维素纤维．     

油气开采过程中CO2腐蚀控制措施探讨

针对油气田严重的CO2腐蚀问题,人们提出了各种各样的防腐蚀措施。其中,应用缓蚀剂进行腐蚀防护已被大家公认为是一种经济有效的防腐措施。本文分析了腐蚀预测和腐蚀监测对防腐工作的重要性和可行性,介绍了常用的几种防腐措施,并着重分析了缓蚀剂防腐措施的有效性。