Kolloide Lösungen von Naphthalin

Ohne Zusammenfassung Uebersetzt von Hans Erbring (Leipzig).     

Diastereoselective spiroannulation of phenolic substrates: synthesis of (+/-)-2-tert-butyl-6-methoxy-1-oxaspiro[4,5]deca-6,9-diene-8-one

The synthesis of a new spiroether is described. The title compound is obtained as a diastereomeric mixture in 45% yield.     

New 64Cu PET imaging agents for personalised medicine and drug development using the hexa-aza cage, SarAr

The success of positron emission tomography (PET) in personalised medicine and drug development requires radioisotopes that provide high quality images and flexible chemistry for a broad application. 64Cu is arguably one of the most suitable PET isotopes for imaging with the evolving target agents, but there are not many appropriate chelating agents for 64Cu and this has limited its wider application. The bi-functional chelator, SarAr is known to bind 64Cu2+ quantitatively (i.e. one metal per ligand present) and rapidly (<2 min) at 10(-6) M over a range of pH (4-9). In this paper the conjugation of SarAr to the whole and fragmented antibody is described. Conjugation of the SarAr to the protein does not impair its coordination of the 64Cu. It complexes the 64Cu2+ rapidly, quantitatively and essentially irreversibly at pH 5. Animal studies show that the 64Cu-SarAr-immunoconjugates maintain their specificity for the target and are stable in vivo. Also, SarAr is a platform technology, is easy to use in a kit formulation and is readily adaptable for the wider application in 64Cu PET imaging.     

Optimization of plasmonic heating by gold nanospheres and nanoshells

Gold nanoparticles have strong and tunable absorption peaks in their optical extinction spectra, a phenomenon that has recently been exploited to generate localized heating in the vicinity of these particles. However the optimum particle geometry and illumination regime to maximize these effects appears not to have been previously examined in any detail. Here we show that the interplay between the particles' absorption cross-sections, volume, and surface area lead to there being specific conditions that can maximize particle temperature and surface heat flux. Optical absorption efficiencies were calculated from the formulation of Mie, and radiative, convective, and conductive heat transfer models were used to model the thermal performance of particles in different situations. Two technologically relevant scenarios for illumination, namely, irradiation by sunlight at 800 W/m2 and by a monochromatic laser source of 50 kW/m2 tuned to the peak absorption wavelength, were considered. For irradiation by sunlight, the resultant heat flux is optimized for an 80 nm diameter nanoshell with an aspect ratio of 0.8, while for irradiation by laser the maximum heat flux is found for 50 nm nanoshells, with an aspect ratio of 0.9.     

Clustering of Patients’ Trajectories with an Auto-Stopped Bisecting K-Medoids Algorithm

Nowadays, long wait, cancellations and resource overload frequently occur in healthcare, especially in those sectors related to the patients passing through the operating theatre in both United States and the European Union. Since more and more hospitals seek to develop the overall patient pathways instead of the effectiveness of “isolated” departments, the most important work has been defining suitable patient groups for employing process management and simulation tools developed in the recent decades. In this study, we proposed a data mining method, an auto-stopped Bisecting K-Medoids clustering algorithm, to classify patients into groups with homogenous trajectories. This method classifies the patient trajectories with two stages. At the first stage, patients are classified by the complexity of outpatient visits; afterwards, the groups obtained at the first stage are further classified by the original information of the trajectories where all medical appointments including outpatient ones are taken into account. By using a real data set collected from a medium-size Belgian hospital, we demonstrate how the proposed approach works and examine which kinds of trajectories are grouped into the same clusters. According to the experimental results, the proposed method can be used to classify patients into manageable groups with homogenous trajectories, which can be used as a base for the process modelling techniques and simulation tools.     

Design and Use of de novo Cascades for the Biosynthesis of New Benzylisoquinoline Alkaloids

The benzylisoquinoline alkaloids (BIAs) are an important group of secondary metabolites from higher plants and have been reported to show significant biological activities. The production of BIAs through synthetic biology approaches provides a higher‐yielding strategy than traditional synthetic methods or isolation from plant material. However, the reconstruction of BIA pathways in microorganisms by combining heterologous enzymes can also give access to BIAs through cascade reactions. Most importantly, non‐natural BIAs can be generated through such artificial pathways. In the current study, we describe the use of tyrosinases and decarboxylases and combine these with a transaminase enzyme and norcoclaurine synthase for the efficient synthesis of several BIAs, including six non‐natural alkaloids, in cascades from l ‐tyrosine and analogues.