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51.
为了开发β受体阻断剂新药(S)-噻吗洛尔半水合物,采用3-吗啉-4-氯-1,2,5-噻二唑为起始原料,经水解反应得到中间体1(3-吗啉-4-羟基-1,2,5-噻二唑)。中间体1与R-环氧氯丙烷发生醚化反应,经后处理及重结晶得到中间体2 {(R)-4-[4-(环氧乙烷-2-基甲氧基)-1,2,5-噻二唑-3-基]吗啉}。中间体2经胺化反应、马来酸成盐及重结晶得到(S)-马来酸噻吗洛尔。(S)-马来酸噻吗洛尔经游离、纯水转晶得到符合药典标准的(S)-噻吗洛尔半水合物,总收率14.05%且e.e.值为99.66%。最终成品经IR、1H-NMR、13C-NMR、MS、TGA、DSC表征,并优化各步反应条件。结果表明:以三乙胺为醚化反应缚酸剂75 ℃反应最佳;以乙醇为胺化反应溶剂46 ℃反应16 h最佳;S-噻吗洛尔的转晶拆分以水作溶剂,比传统不对称合成工艺安全稳定,操作简单,适合工业化生产。 相似文献
52.
Although greedy algorithms possess high efficiency, they often receive suboptimal solutions of the ensemble pruning problem, since their exploration areas are limited in large extent. And another marked defect of almost all the currently existing ensemble pruning algorithms, including greedy ones, consists in: they simply abandon all of the classifiers which fail in the competition of ensemble selection, causing a considerable waste of useful resources and information. Inspired by these observations, an interesting greedy Reverse Reduce-Error (RRE) pruning algorithm incorporated with the operation of subtraction is proposed in this work. The RRE algorithm makes the best of the defeated candidate networks in a way that, the Worst Single Model (WSM) is chosen, and then, its votes are subtracted from the votes made by those selected components within the pruned ensemble. The reason is because, for most cases, the WSM might make mistakes in its estimation for the test samples. And, different from the classical RE, the near-optimal solution is produced based on the pruned error of all the available sequential subensembles. Besides, the backfitting step of RE algorithm is replaced with the selection step of a WSM in RRE. Moreover, the problem of ties might be solved more naturally with RRE. Finally, soft voting approach is employed in the testing to RRE algorithm. The performances of RE and RRE algorithms, and two baseline methods, i.e., the method which selects the Best Single Model (BSM) in the initial ensemble, and the method which retains all member networks of the initial ensemble (ALL), are evaluated on seven benchmark classification tasks under different initial ensemble setups. The results of the empirical investigation show the superiority of RRE over the other three ensemble pruning algorithms. 相似文献
53.
Cheese fortification using saturated monoglyceride self‐assembly structures as carrier of omega‐3 fatty acids
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Sonia Calligaris Alexandra Ignat Marialuisa Biasutti Nadia Innocente Maria Cristina Nicoli 《International Journal of Food Science & Technology》2015,50(9):2129-2134
The purpose of this research was to study the capacity of emulsions containing saturated monoglyceride self‐assembly structures to deliver omega‐3 fatty acids in fresh soft cheese. To this aim, fortified emulsions containing different ratios of milk, saturated monoglycerides (MGs) and cod liver oil were added to milk before cheese‐making. These emulsions were characterised by distinct microstructural features observed by polarised light microscopy and apparent viscosity values. The omega‐3 delivery performance of MG emulsions highlighted that this strategy allowed a good retention of the omega‐3‐rich oil in the curd (up to 75%). The fortified cheeses showed yield value and fat content higher than those of control samples. The enriched cheese showed hardness and cohesiveness obtained by texture profile analysis similar to those of the unfortified product. Only a slight decrease in gumminess was detected in fortified cheese. 相似文献
54.
Characteristics and formation mechanism of porosities in CFRP during laser joining of CFRP and steel
An experimental investigation on the mechanism of porosity formation during the laser joining of carbon fiber reinforced polymer (CFRP) and steel is presented. The porosity morphology and distribution were characterized by optical and scanning electron microscopy, and the thermal pyrolysis behaviors were investigated by thermal analysis and designed back-side cooling experiments. The results show that there are two types of porosities in CFRP. Porosity I only appears when the heat input is more than 77.8 J/mm. It has a smooth inner wall and distributes near the bonding interface between CFRP and steel at the central area of melted zone, which is caused by gaseous products such as CO2, NH3, H2O, and hydrocarbons produced by the pyrolysis of CFRP. Porosity II can be seen under all joining conditions. It has a rough inner wall and distributes far away from the bonding interface, concentrating at the final solidification locations. Porosity II is caused by the shrinkage of melted CFRP during solidification stage. 相似文献
55.
Akira Yamamoto Kentaro Teramura Saburo Hosokawa Tsunehiro Tanaka 《Science and Technology of Advanced Materials》2015,16(2)
The effect of SO2 gas was investigated on the activity of the photo-assisted selective catalytic reduction of nitrogen monoxide (NO) with ammonia (NH3) over a TiO2 photocatalyst in the presence of excess oxygen (photo-SCR). The introduction of SO2 (300 ppm) greatly decreased the activity of the photo-SCR at 373 K. The increment of the reaction temperature enhanced the resistance to SO2 gas, and at 553 K the conversion of NO was stable for at least 300 min of the reaction. X-ray diffraction, FTIR spectroscopy, thermogravimetry and differential thermal analysis, x-ray photoelectron spectroscopy (XPS), elemental analysis and N2 adsorption measurement revealed that the ammonium sulfate species were generated after the reaction. There was a strong negative correlation between the deposition amount of the ammonium sulfate species and the specific surface area. Based on the above relationship, we concluded that the deposition of the ammonium sulfate species decreased the specific surface area by plugging the pore structure of the catalyst, and the decrease of the specific surface area resulted in the deactivation of the catalyst. 相似文献
56.
通过制备不同晶相结构〔单斜相(m-ZrO_2)、四方相(t-ZrO_2)和无定型(a-ZrO_2)〕ZrO_2载体,再通过沉积沉淀法制得Cu/m-ZrO_2、Cu/t-ZrO_2和Cu/a-ZrO_2催化剂,分别用于催化二乙醇胺脱氢合成亚氨基二乙酸反应。采用XRD、氮气物理吸附脱附、XPS、H_2-TPR、CO_2-TPD对催化剂的结构进行了表征。结果表明,Cu/m-ZrO_2催化剂界面更加有利于Cu~+/Cu~0稳定存在,具有更多的碱性位点,且抗氧化性较好。在二乙醇胺脱氢反应中,Cu/m-ZrO_2催化剂性能最好,反应时间为2.5 h,亚氨基二乙酸收率为97.64%。 相似文献
57.
《International Journal of Hydrogen Energy》2020,45(57):32856-32864
The electrode ionomer is a key factor that significantly affects the catalyst layer morphology and fuel cell performance. Herein, sulfonated poly(arylene ether sulfone)-based electrode ionomers with polymers of various molecular weights and alcohol/water mixtures were prepared, and those comprising the alcohol/water mixture showed a higher performance than the ones prepared using higher boiling solvents, such as dimethylacetamide; this is owing to the formation of the uniformly dispersed ionomer catalyst layer. The relation between ionomer molecular weight for the same polymer structure and the sulfonation degree was investigated. Because the chain length of polymer varies with molecular weight and chain entanglement degree, its molecular weight affects the electrode morphology. As the ionomer covered the catalyst, the agglomerates formed were of different morphologies according to their molecular weight, which could be deduced indirectly through dynamic light scattering and scanning electron microscopy. Additionally, the fuel cell performance was confirmed in the current-voltage curve. 相似文献
58.
《Journal of the European Ceramic Society》2020,40(8):2731-2745
Thermal barrier coatings (TBCs) play a pivotal role in protecting the hot structures of modern turbine engines in aerospace as well as utility applications. To meet the increasing efficiency of gas turbine technology, worldwide research is focused on designing new architecture of TBCs. These TBCs are mainly fabricated by atmospheric plasma spraying (APS) as it is more economical over the electron beam physical vapor deposition (EB-PVD) technology. Notably, bi-layered, multi-layered and functionally graded TBC structures are recognized as favorable designs to obtain adequate coating performance and durability. In this regard, an attempt has been made in this article to highlight the structure, characteristics, limitations and future prospects of bi-layered, multi-layered and functionally graded TBC systems fabricated using plasma spraying and its allied techniques like suspension plasma spray (SPS), solution precursor plasma spray (SPPS) and plasma spray –physical vapor deposition (PS-PVD). 相似文献
59.
Alexandra Kodadová Zuzana Vitková Petra Herdová Anton Ťažký Jarmila Oremusová Daniel Grančai 《Drug development and industrial pharmacy》2015,41(7):1080-1088
This study deals with the formulation of natural drugs into hydrogels. For the first time, compounds from the sage essential oil were formulated into chitosan hydrogels. A sample preparation procedure for hydrophobic volatile analytes present in a hydrophilic water matrix along with an analytical method based on the gas chromatography coupled with the mass spectrometry (GC-MS) was developed and applied for the evaluation of the identity and quantity of essential oil components in the hydrogels and saline samples. The experimental results revealed that the chitosan hydrogels are suitable for the formulation of sage essential oil. The monoterpene release can be effectively controlled by both chitosan and caffeine concentration in the hydrogels. Permeation experiment, based on a hydrogel with the optimized composition [3.5% (w/w) sage essential oil, 2.0% (w/w) caffeine, 2.5% (w/w) chitosan and 0.1% (w/w) Tween-80] in donor compartment, saline solution in acceptor compartment, and semi-permeable cellophane membrane, demonstrated the useful permeation selectivity. Here, (according to lipophilicity) an enhanced permeation of the bicyclic monoterpenes with antiflogistic and antiseptic properties (eucalyptol, camphor and borneol) and, at the same time, suppressed permeation of toxic thujone (not exceeding its permitted applicable concentration) was observed. These properties highlight the pharmaceutical importance of the developed chitosan hydrogel formulating sage essential oil in the dermal applications. 相似文献
60.
王学鹏 《电子制作.电脑维护与应用》2015,(6)
CAN-BUS系统自问世以来,已将近30年,当代各品牌车辆纷纷采用,但大部分技术人员对CAN总线系统既熟悉又陌生。经常能听到,但具体操作又显得有些力不从心。本文通过对奇瑞A3品牌轿车CAN总线的巧妙应用,引导大家进一步理解和应用CAN总线。 相似文献