Regioselective Introduction of Electrophiles into Piperidine Derivatives at the 4-Position

Regioselective introduction of various electrophiles (aldehydes, ketones, and imines) into piperidine skeleton at the 4-position was achieved with a catalytic amount of Pd(OAc)2/PPh3 in the presence of excess Et2Zn. In addition, enantioselective introduction of benzaldehyde into piperidine derivatives was accomplished by using chiral phosphine ligand with moderate enantioselectivity

Seismic characterisation of the subsoil under a historic building: Cathedral Church of Saint Mary in Murcia case study

This research focuses on the Cathedral Church of Saint Mary in Murcia, Spain, which is located in a moderate-to-high seismic risk zone in the Spanish context. The study uses geophysical techniques and geotechnical investigation to characterise seismic ground models at the building's scale, aiming to understand the real amplification of the ground under seismic effect in historic buildings. Three soil layers (silt, sand with gravel, and gravel) were identified through core borings. Multichannel Analysis of Surface Waves (MASW) profiles and Mini-array profiles revealed Vs values of 305 ± 32 m/s, 296 ± 62 m/s, and 440 ± 38.5 m/s, respectively, for these materials. Seismic Refraction Tomography (SRT) showed Vp values of 586 ± 73 m/s, 700 m/s, and 1466 ± 489 m/s for the corresponding layers. The horizontal-to-vertical spectral ratio (HVSR) approach identified a ground predominant period ranging from 0.37 to 0.38 s. Another significant peak at 2.3 s is observed, probably associated to the Triassic basement. Three seismic events with magnitudes Mw between 4.9 and 5.1 were used as inputs to determine the amplification factor (AF). The results indicate a PGA amplification factor between 1.7 and 2.1. These results contribute to the conservation and mitigation of seismic risk of this cultural heritage generating input data that enables precise computation of the soil-structure interaction

Feasibility study of immediate pharyngeal cooling initiation in cardiac arrest patients after arrival at the emergency room

AIM: Cooling the pharynx and upper oesophagus would be more advantageous for rapid induction of therapeutic hypothermia since the carotid arteries run in their vicinity. The aim of this study was to determine the effects of pharyngeal cooling on brain temperature and the safety and feasibility for patients under resuscitation. METHODS: Witnessed non-traumatic cardiac arrest patients (n=108) were randomized to receive standard care with (n=53) or without pharyngeal cooling (n=55). In the emergency room, pharyngeal cooling was initiated before or shortly after return of spontaneous circulation by perfusing physiological saline (5 °C) into a pharyngeal cuff for 120 min. RESULTS: There was a significant decrease in tympanic temperature at 40 min after arrival (P=0.02) with a maximum difference between the groups at 120 min (32.9 ± 1.2°C, pharyngeal cooling group vs. 34.1 ± 1.3°C, control group; P<0.001). The return of spontaneous circulation (70% vs. 65%, P=0.63) and rearrest (38% vs. 47%, P=0.45) rates were not significantly different based on the initiation of pharyngeal cooling. No post-treatment mechanical or cold-related injury was observed on the pharyngeal epithelium by macroscopic observation. The thrombocytopaenia incidence was lower in the pharyngeal cooling group (P=0.001) during the 3-day period after arrival. The cumulative survival rate at 1 month was not significantly different between the two groups. CONCLUSIONS: Initiation of pharyngeal cooling before or immediately after the return of spontaneous circulation is safe and feasible. Pharyngeal cooling can rapidly decrease tympanic temperature without adverse effects on circulation or the pharyngeal epithelium

Elevated Intraocular Pressure, Optic Nerve Atrophy, and Impaired Retinal Development in ODAG Transgenic Mice

PURPOSE. In an earlier study, a cDNA was cloned that showed abundant expression in the eye at postnatal day (P)2 but was downregulated at P10; it was named ODAG (ocular development-associated gene). Its biological function was examined by generating and analyzing transgenic mice overexpressing ODAG (ODAG Tg) in the eye and by identifying ODAG-binding proteins. METHODS. Transgenic mice were generated by using the mouse Crx promoter. EGFP was designed to be coexpressed with transgenic ODAG, to identify transgene-expressing cells. Overexpression of ODAG was confirmed by Northern and Western blot analysis. IOP was measured with a microneedle technique. The eyes were macroscopically examined and histologically analyzed. EGFP expression was detected by confocal microscope. Proteins associated with ODAG were isolated by pulldown assay in conjugation with mass spectrometry. RESULTS. Macroscopically, ODAG Tg exhibited gradual protrusion of the eyeballs. The mean IOP of ODAG Tg was significantly higher than that of wild-type (WT) littermates. Histologic analysis exhibited optic nerve atrophy and impaired retinal development in the ODAG Tg eye. EGFP was expressed highly in the presumptive outer nuclear layer and weakly in the presumptive inner nuclear layer in the ODAG Tg retina. Rab6-GTPase-activating protein (Rab6-GAP) and its substrate, Rab6, were identified as ODAG-binding proteins. CONCLUSIONS. Deregulated expression of ODAG in the eye induces elevated intraocular pressure and optic nerve atrophy and impairs retinal development, possibly by interfering with the Rab6/Rab6-GAP-mediated signaling pathway. These results provide new insights into the mechanisms regulating ocular development, and ODAG Tg would be a novel animal model for human diseases caused by ocular hypertension. (Invest Ophthalmol Vis Sci. 2009;50:242-248) DOI:10.1167/iovs.08-2206 O cular development is a complex process, involving several genes with expression that is strictly controlled in a spatial and temporal manner. Although several genes, including Pax6, Rx, and Crx, are essential for normal ocular formation, 1-3 the molecular mechanism(s) governing eye development has not been fully elucidated. To identify genes that are preferentially expressed in the developing eye, we performed a differential display using mRNAs extracted from postnatal day (P)2 and P10 mouse eyes. 4 At P2, ODAG was highly expressed in all the retinal layers (presumptive outer nuclear layer [ONL], presumptive inner nuclear layer [INL], and ganglion cell layer [GCL]), but at P7, its expression decreases, especially in the GCL, and at P14, no apparent expression is detected. To investigate, we generated transgenic mice overexpressing ODAG (ODAG Tg). The mouse Crx promoter, which directs transgene expression in photoreceptors, From th

Efficient oxidation of alcohols electrochemically mediated by azabicyclo-N-oxyls

Preparation of azabicyclo-N-oxyls and the electrochemical oxidation of alcohols using them as mediators have been exploited. This oxidation was applicable to a transformation of sterically hindered secondary alcohols into the corresponding ketones in high yields