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111.
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
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Cheese fortification using saturated monoglyceride self‐assembly structures as carrier of omega‐3 fatty acids 下载免费PDF全文
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
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The study presents the preparation of the new magnetic nanocomposite based on PLGA and magnetite. The PLGA used to obtain the magnetic nanocomposites was synthesized by the copolymerization of lactic acid with glycolic acid, in the presence of tin octanoate [Sn(Oct)2] as catalyst, by polycondensation procedure. Magnetite was obtained by co-precipitation from aqueous salt solutions FeCl2/FeCl3. The particles size of magnetite was 420 nm, and the saturation magnetization 62.78 emu/g, while the PLGA/magnetite nanocomposite size was 864 nm and the saturation magnetization 39.44 emu/g. The magnetic nanocomposites were characterized by FT-IR, DLS technique, SEM, VSM and simultaneous thermal analyses (TG–FTIR–MS). The polymer matrix PLGA acts as a shell and carrier for the active component, while magnetite is the component which makes targeting possible by external magnetic field manipulation. Based on the gases resulted by thermal degradation of PLGA copolymer, using the simultaneous analysis TG–FTIR–MS, a possible degradation mechanism was proposed. 相似文献
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A small handful of recent studies have addressed a phenomenon known as “phantom vibration syndrome”. This refers to when phone users perceive their device to vibrate, indicating that a call or text is incoming, when in fact the phone did not vibrate at all. Though these studies show that most users do not find phantom vibration hallucinations to be very bothersome, they also find that a large majority of users experience this phenomenon. This paper explores what the striking prevalence of phantom vibration syndrome means for our contemporary relationships with technology. I begin with a review of the theories purporting to explain these data, which largely rely on particular understandings of the brain. Next I develop an alternative theory of phantom vibration syndrome based on insights from the philosophical tradition of phenomenology. This account considers the ways users develop bodily and perceptual habits regarding how the phone is understood and used. By critically contrasting these different theories, we can refine our questions about what the high prevalence of phantom vibration syndrome implies about our contemporary technological situation. 相似文献
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In recent years, many tidal turbine projects have been developed using composites blades. Tidal turbine blades are subject to ocean forces and sea water aggressions, and the reliability of these components is crucial to the profitability of ocean energy recovery systems. The majority of tidal turbine developers have preferred carbon/epoxy blades, so there is a need to understand how prolonged immersion in the ocean affects these composites. In this study the long term behaviour of different carbon/epoxy composites has been studied using accelerated ageing tests. A significant reduction of composite strengths has been observed after saturation of water in the material. For longer immersions only small further changes in these properties occur. No significant changes have been observed for moduli nor for composite toughness. The effect of sea water ageing on damage thresholds and kinetics has been studied and modelled. After saturation, the damage threshold is modified while kinetics of damage development remain the same. 相似文献
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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
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