Stereoselective synthesis of tetrahydropyran-3-ones by rearrangement of oxonium ylides generated from metal carbenoids

The synthesis of tetrahydropyran-3-ones by copper-catalysed reactions of diazo ketone tethered allylic ethers has been explored. Product distribution can be explained by the intermediacy of a free ylide or direct rearrangement of a metal-bound ylide equivalent.     

Facile radiosynthesis of <Superscript>18</Superscript>F-labeled β-glutamic acid as a new PET tracer for imaging lung cancer

In this paper, N-(2-[¹⁸F]fluoropropionyl)-β-glutamic acid 8 ([¹⁸F]FP-β-Glu), a new N-substituted ¹⁸F-labeled amino acid tracer, was synthesized from the precursor 4 (diethyl 3-(2-bromopropanamido)pentanedioate) via a two-step reaction on the modified FDG synthesizer. The radiochemical yield was 20 ± 5% (n = 10, decay-corrected) from [¹⁸F]fluoride within 40 min, the radiochemical purity was 98%. Moreover, microPET studies showed that [¹⁸F]FP-β-Glu 8 exhibited rapid tumor uptake and good tumor-to-lung ratio in SPC-A-1 tumor-bearing mice. A high accumulation of radioactivity was found in the kidneys and bladder, which suggested that the tracer was mainly eliminated through the urinary system.     

正电子发射显像剂O-(2-[18F]氟乙基)-L-酪氨酸的新型前体的合成

设计合成了5种新型正电子发射断层显像剂[O-(2-[¹⁸F]氟乙基)-L-酪氨酸的前体化合物：N-叔丁氧羰基-O-(2-甲磺酰/对硝基苯磺酰)-氧乙基-L-酪氨酸甲酯(9a,11a)和N-叔丁氧羰基-O-(2-甲磺酰/对甲苯磺酰/对硝基苯磺酰)-氧乙基-L-酪氨酸叔丁酯(9b,10b,11b)。 这些化合物以L-酪氨酸为原料,先与甲醇发生酯化反应或与乙酸叔丁酯进行酯交换,再用叔丁氧羰基保护氨基,最后以碳酸钾为碱、18-冠-6为相转移催化剂与乙二醇的磺酸酯在丙酮溶液中加热回流形成目标化合物,总收率为30%～67%。     

Large N Duality, Lagrangian Cycles, and Algebraic Knots

We consider knot invariants in the context of large N transitions of topological strings. In particular we consider aspects of Lagrangian cycles associated to knots in the conifold geometry. We show how these can be explicitly constructed in the case of algebraic knots. We use this explicit construction to explain a recent conjecture relating study of stable pairs on algebraic curves with HOMFLY polynomials. Furthermore, for torus knots, using the explicit construction of the Lagrangian cycle, we also give a direct A-model computation and recover the HOMFLY polynomial for this case.     

Influence of the addition of aluminium nanoparticles on thermo-rheological properties of hydroxyl-terminated polybutadiene-based composite propellant and empirical modelling

The heat transfer performance and entropy analysis are done in a compact loop heat pipe (CLHP) with Al₂O₃/water and Ag/water nanofluid. A compact loop heat pipe having a flat square evaporator with dimensions of 34 mm (L)?×?34 mm (W)?×?19 mm (H) has been fabricated and tested for the heat load ranging from 30 to 500 W. The experimental tests are conducted by keeping the CLHP in the vertical orientation with distilled water, silver (Ag)/water and aluminium oxide (Al₂O₃)/water nanofluid having low volume concentrations of (0.09% and 0.12%). The effect of wall and vapour temperature, evaporator and condenser heat transfer coefficient, thermal resistance on the applied heat loads is experimentally investigated and compared. The experimental results showed that the evaporator thermal resistance is reduced by 34.70% and 20.21%, respectively, for 0.12 vol% of Ag, Al₂O₃ nanoparticles when compared with that of the distilled water. For the same volume concentrations of Ag, Al₂O₃ nanoparticles, an enhancement of 34.52%, 23.7%, 39.27% and 30.8%, respectively, observed for the convective heat transfer coefficients at the evaporator and condenser. The entropy is also reduced by 19.08% and 11.58% when Ag and Al₂O₃ nanofluids are used as the operating fluid. From the experimental tests, it is found that the addition of small amount of Ag nanoparticles in the working fluid enhanced the operating range by 15% when compared with that of Al₂O₃/water nanofluid without the occurrence of any dry-out conditions.

     

Recent Advances Utilized in the Recycling of Homogeneous Catalysis

Homogeneous catalysts often show high activity and selectivity towards the various chemical transformations. Most of the transition metal‐based active catalysts are expensive, rare, and have strict regulations for their use in pharmaceutical products. Hence, there is a requirement to develop suitable technologies for the practical separation and recycling of metal complex catalysts along with the sustainability of the process. This review focuses on the recent techniques used for the catalyst separation, their recovery, and recyclability of the homogeneous form of catalysts based on their economic compatibility and industrial applications. Various homogeneous catalysts have been reviewed on the basis of their support or media, active centres and recyclability aspects of the catalysts. This review gives brief insights into the varied examples of different recycling techniques utilized in the past 6–7 years.     

Physicochemical Investigation of Engineered Nanosuspensions Containing Model Drug,Lansoprazole

Lansoprazole is a proton-pump inhibitor used in treatment of gastric ulcers, gastroesophageal reflux disease (GERD), and Zollinger–Ellison syndrome. The objective of the study was physicochemical investigation and comparative characterization of nanosuspensions of lansoprazole by complexing with β-cyclodextrin and β-cyclodextrin-based nanosponges to enhance its solubility and stability. Inclusion complexes of lansoprazole with β-cyclodextrin and nanosponges were prepared by physical method and polymer condensation method, respectively. Particle size, zeta potential, encapsulation efficiency, in vitro release, FTIR, and Differential Scanning Calorimeter (DSC) studies were used as characterization parameters. The average particle size of lansoprazole nanoparticles was found to be in the range of 178.7 ± 6.39 nm to 204.9 ± 2.91 nm. The high zeta potential values were attained to ensure a high-energy barrier and favor a good stability of nanosuspensions. In vitro release study showed the controlled release of lansoprazole, which was more satisfactory than individual drug. FTIR spectroscopy showed that there was interaction of cyclodextrin and its nanosponges with drug. DSC study revealed that drug was involved in complexion with cyclodextrin and nanosponges. Solubility and stability of lansoprazole were remarkably improved by inclusion complexation. Based on these findings, it can be concluded that engineered nanosuspension of lansoprazole is a promising carrier for nanoparticulate drug delivery in gastric ulcer.     

Fracto-mechanoluminescence and mechanics of fracture of solids

The present paper explores the correlation between fracto-mechanoluminescence and fracture of solids and thereby provides a clear understanding of the physics of fracto-mechanoluminescence. When a fluorescent or non-photoluminescent crystal is fractured impulsively by dropping a load on it, then initially the mechanoluminescence (ML) intensity increases linearly with time, attains a maximum value I_m at a particular time t_m and later on it decreases exponentially with time. However, when a phosphorescent crystal is fractured impulsively by dropping a load on it, then initially the ML intensity increases linearly with time, attains a maximum value I_m at a particular time t_m and later on it decreases initially at a fast rate and then at a slow rate. For low impact velocity the value of t_m is constant, however, for higher impact velocity t_m decreases logarithmally with the increasing impact velocity. Whereas the peak ML intensity I_m increases linearly with the impact velocity, the total ML intensity I_T, initially increases linearly with the impact velocity and then it tends to attain a saturation value for higher values of the impact velocity. The value of t_m increases logarithmally with the thickness of crystals, I_m increases linearly with the area of cross-section of crystals and I_T increases linearly with the volume of crystals. Generally, the ML of non-irradiated crystals decreases with increasing temperature of crystals. Depending on the prevailing conditions the ML spectra consist of either gas discharge spectra or solid state luminescence spectra or combination of the both. On the basis of the rate of generation of cracks and the rate of creation of new surface area of crystals, expressions are derived for the ML intensity and they are found to explain satisfactorily the temporal, spectral, thermal, crystal-size, impact velocity, surface area, and other characteristics of ML. The present investigation may be useful in designing of damage sensors, fracture sensors, ML-based safety management monitoring system, fuse-system for army warheads, milling machine, etc. The present study may be helpful in understanding the processes involved in earthquakes, earthquake lights and mine-failure as they basically involve fracture of solids.     

Distributed Online Frequency Assignment in Cellular Networks

A cellular network is generally modeled as a subgraph of the triangular lattice. The distributed online frequency assignment problem can be abstracted as a multicoloring problem on a weighted graph, where the weight vector associated with the vertices models the number of calls to be served at the vertices and is assumed to change over time. In this paper, we develop a framework for studying distributed online frequency assignment in cellular networks. We present the first distributed online algorithms for this problem with proven bounds on their competitive ratios. We show a series of algorithms that use at each vertex information about increasingly larger neighborhoods of the vertex, and that achieve better competitive ratios. In contrast, we show lower bounds on the competitive ratios of some natural classes of online algorithms.     

Adsorption of Metformin on Graphene Nanoribbons and Application in Treatment of Oral Cancer Using Photothermal Energy

Graphene nanoribbons are thin sheets of graphene showing exclusive characteristics such as better drug-loading capacity, adsorption on mammalian cells, greater surface area, and light-absorbing ability. The current research work is to develop metformin-adsorbed carboxyl-functionalized oxidized graphene nanoribbons and utilize drug repurposing for the treatment of oral cancer by activating photo-thermal radiation therapy. The nanoribbons are formulated by Hummer's method and evaluated for several characterization parameters like ATR- Fourier Transform Infrared (FTIR), Differential scanning calorimetry (DSC), topology, in vitro efficacy, ex vivo and in vitro cell line studies. The ATR-FTIR spectrum of formulated nanoribbons shows distinctive peak at 3370 cm⁻¹ ( N H group) of metformin. The DSC specifies the incidence of steep endothermic crests at 235 °C ( C NH₃). The in vitro and ex vivo drug release studies show enhanced drug release in acidic pH (6.4) than physiological pH (7.4) with photothermal radiation. The in vitro cell line studies are processed via two-way ANOVA that exhibits 67.74 ± 0.03% of % inhibition in presence of photothermal radiation. The study demonstrates higher inhibition of cancerous cells at lower concentration of drug and photothermal therapy in comparison to plain drug. The characteristic feature of graphene is used to develop targeted drug delivery system against the oral cancerous cells.