Новий метод синтезу атомоксетину та його взаємодія з азоловмісними сульфохло- ридами

A new approach to the synthesis of atomoxetine using the methods of enzymatic catalysis has been developed;the interaction of atomoxetine with a number of azole-containing heterocyclic sulfochlorides has been studied. Thecarbonyl group of 3-chloro-1-phenyl-propane-1-one was region-specifically reduced with NADPH-dependentcarbonylreductase (SSCR) in phosphate buffer solution. In Mitsunoby reaction with o-methylphenole the inversionof the final product configuration takes place and [R]-1-(3-chloro-1-phenypropoxy)-2-methylbenzene is formed.Its further treatment with methylamine results in the base of atomoxetine, which may be isolated from the solutionas a chloride. In order to develop the novel biologically active compounds the series of sufonyl chlorides withoxazole and isoxazole substituents were reacted with atomoxetine. The sulfonamides obtained fully comply withall criteria for the molecules – candidates for the biomedical study.Разработан метод синтеза атомоксетина с использованием стереоспецифичного ферментативного катализа. Карбонильная группа в структуре 3-хлор-1-фенил-пропан-1-она региоспецифично восстановлена с образованием NADPH-зависимой карбонилредуктазы (SSCR) в фосфатном буфере. В условиях реакции Мицунобу с о-крезолом происходит обращение конфигурации конечного продукта с образованием в ходе реакции [R]-1-(3-хлор-1-фенилпропокси)-2-метилбензола, который далее при обработке метиламином образует основание атомоксетина, выделяемое из раствора в виде соли с хлористоводородной кислотой. С целью поиска новых биологически активных соединений получен ряд сульфохлоридов с оксазольными и изоксазольными заместителями, которые далее вводились в реакцию с атомоксетином. Полученные в работе сульфонамиды удовлетворяют требованиям, предъявляемым к молекулам – кандидатам для биомедицинских исследований.Розроблено метод синтезу атомоксетину з використанням стереоспецифічного ферментативного каталізу. Карбонільна група в структурі 3-хлоро-1-феніл-пропан-1-ону регіоспецифічно відновлена з використанням NADPH-залежної карбонілредуктази (SSCR) в фосфатному буфері. В умовах реакції Міцунобу з о-крезолом відбувається обернення конфігурації кінцевого продукту з утворенням [R]-1-(3-хлоро-1-фенілпропокси)-2-метилбензолу, який далі при обробці метиламіном утворює основу атомоксетину, яка виділяється з розчину у вигляді солі з хлористоводневою кислотою. З метою пошуку нових біологічно активних сполук отримано ряд сульфохлоридів з оксазольними та ізоксазольними замісниками, які далі вводились в реакцію з атомоксетином. Отримані в роботі сульфонаміди відповідають вимогам, які висуваються до молекул – кандидатів для біомедичних досліджень

Dispersed copper (I) oxide particles encapsulated by polylactide

One of the approaches for the production of polymer composite materials with a biocidal effect is based on the use of dispersed particles of some metal oxides as a filler (for example, copper oxide or zinc oxide). Such an approach allows not only providing a biocidal effect, but also increasing such mechanical characteristics as the modulus of elasticity, hardness, and abrasion resistance. The mechanical characteristics of such polymer composite materials can be controlled by formation of a sheath (for example, from polylactide) of a given thickness on the surfaces of dispersed particles. Polylactide is a biodegradable polymer, widely used as coating material for particles with biocidal properties. The parameters of the methods for forming a polylactide sheath are determined by the sheath’s thickness and the sheath’s adhesion to the particle surface. The purpose of the study was to determine the parameters of the polymer sheath’s formation on the surfaces of dispersed submicron copper oxide (I) particles during coacervation of polylactide from the solution. The encapsulation of copper (I) oxide particles was carried out by the coacervation process in a solution. Polylactide was displaced from the solution in benzene by hexane in the presence of copper (I) oxide particles. It was shown that a sheath thickness of about 250 nm can be obtained by using the polylactide sheath formation method. The recommended parameters of the polylactide sheath formation method were determined: solution temperature of 35÷38 °C, hexane volume not more than 30±2 ml. The sheath had weak adhesion to particle surfaces: adhesion was determined by the roughness of the particle surface. The mechanical characteristics of the epoxy resin ED-20 polymer composition filled with the encapsulated particles were considered in the study. The increase in the mechanical properties of the polymer composition with encapsulated particles in comparison with the samples of polymer composition with non-encapsulated particles was revealed. That can indicate the increased adhesion of encapsulated particles to such polymer matrix

The effect of radiation losses in localized fluorescence upon laser pumping of fluorescent random media

Background and Objectives: Excitation of fluorescence upon laser pumping of fluorescent multiple scattering media is a complex process that plays a key role in many applications of modern optics and laser physics, from optical biomedical diagnostics to controlling the parameters of functional materials for photonics and optoelectronics. The effect of radiation losses in local fluorescence emitters, which are associated with laser speckles in pumped random media, on the fluorescence output is considered. Materials and Methods: Within the framework of the concept of an ensemble of statistically independent local fluorescence emitters in a laser-pumped random medium, a model of radiation losses in an arbitrarily chosen local emitter is considered. The model takes into account both an extreme value of the cross section of radiation losses for a single emitter, which depends on its characteristic size and the concentration of fluorophore molecules in the medium, and the effect of radiation exchange with other emitters. The scattering properties of a laser-pumped fluorescent medium are considered as a suppressing factor for the ballistic radiation transfer between the local emitters. The modeled results are compared to the previously obtained empirical data on the effective cross section of radiation losses for Rhodamine-6G-saturated layers of close-packed anatase nanoparticles under pulsed laser pumping at the wavelength of 532 nm. Results: The relationship between the effective cross section of radiation losses and the characteristic size of the emitters, the concentration of fluorophore molecules, and the mean scattering free path of fluorescent radiation was obtained. It was found within the framework of the considered model that both the characteristic size of local emitters and the reduction factor to the cross section of radiation losses due to light transfer from other emitters are practically independent of the pump intensity, with the exception of a narrow interval of low intensities. On the other hand, the scattering length significantly affects these characteristics due to the “screening” effect in the case of expressed multiple scattering. Conclusion: Radiation exchange between local stochastic emitters of fluorescence radiation in laser-pumped random media is one of the key factors controlling the fluorescence response of the medium with increasing pump intensity. The considered phenomenological model makes it possible to adequately interpret the experimentally observed features of the behavior of the effective cross section of radiation losses for these systems. The obtained results can be used as a physical basis for the development of new approaches to laser probing of random media in terms of the interpretation of the experimental data

Formation of an Axisymmetric Swirling Flow in a Cyclone-Vortex Pre-Heating with a Capacity of 65 MW

Представлены энергообъекты с котельным оборудованием, оснащенным циклонно-вихревыми предтопками мощностью 65 МВт. Рассмотрены конструктивные отличия циклонно-вихревых предтопков с односторонним и четырехсторонним подводом газообразного топлива в камеру сгорания. Описан принцип работы циклонно-вихревого предтопка и особенности распределения воздушной и газовой сред в камере сгорания. Приведена схема расположения экспериментальных сечений в циклонно-вихревых предтопках для проведения пневмометрических исследований, дан перечень параметров, замеренных при исследованиях, а также информация по режимам и нагрузкам котлов. Показаны результаты пневмометрических исследований. Приведены графики изменения параметров закрученного потока в циклонно-вихревых предтопках при горении и без горения природного газа. Оценено влияние одностороннего и четырехстороннего ввода природного газа в камеру сгорания циклонно-вихревого предтопка на формирование симметричного закрученного потока. Сравнительный анализ параметров закрученного потока показал величину отклонения его аэродинамической оси от геометрической оси камеры сгорания. По профилю изменения тангенциальной составляющей вектора полной скорости отмечены области формирования закрученного потока при горении и без горения газа. Выявлено влияние аксиального ввода воздуха на процесс горения и изменение температуры закрученного потока. Анализ данных по содержанию кислорода и значениям температур «горячего» потока показал области горения и области смешения воздуха и газа в камере сгорания циклонно-вихревого предтопка. Представленные выводы указывают на то, что равномерное распределение газа через все тангенциальные воздушные вводы в процессе горения позволяет интенсифицировать тепло- и массообмен топлива и воздуха и добиться практически полного сгорания газа в объёме камеры сгорания циклонно-вихревого предтопка с последующим догоранием в топке котла.The article presents power facilities with boiler equipment equipped with cyclone-vortex preheaters with a capacity of 65 MW. The design differences of cyclone-vortex preheaters with one-sided and four-sided supply of gaseous fuel to the combustion chamber are considered. The principle of operation of the cyclone-vortex pre-heating, the features of the distribution of air and gas media in the combustion chamber of the cyclone-vortex pre-heating are described. The article presents a diagram of the location of experimental sections in cyclone-vortex pre-furnaces for conducting pneumometric studies, a list of parameters measured during research is given, information on the modes and loads of boilers during research is given. The results of pneumometric studies are presented. Graphs of changes in the parameters of the swirling flow in cyclone-vortex preheaters during gorenje and without gorenje of natural gas are given. The influence of one-sided and four-sided input of natural gas into the combustion chamber of cyclone-vortex pre-heating on the formation of a symmetrical swirling flow is estimated. A comparative analysis of the parameters of the swirling flow showed the magnitude of the deviation of the aerodynamic axis of the swirling flow from the geometric axis of the combustion chamber of the cyclone-vortex pre-tank. According to the profile of the change in the tangential component of the full velocity vector, the regions of the formation of a swirling flow during combustion and without gorenje gorenje gas in the combustion chamber of the cyclone-vortex pre-heating are marked. The influence of axial air input on the combustion process and the temperature change of the swirling flow is revealed. Gorenje Analysis of data on oxygen content and temperature values of the «hot» flow showed the areas of gorenje and the areas of mixing of air and gas in the combustion chamber of the cyclone-vortex pre-heating. The presented conclusions indicate that the uniform distribution of gas through all tangential air inlets during the combustion process allows to intensify the heat and mass exchange of fuel and air and achieve almost complete combustion of gas in the volume of the combustion chamber of cyclone-vortex pre-heating with subsequent gorenje in the boiler furnac

Ocrelizumab versus Interferon Beta-1a in Relapsing Multiple Sclerosis

Supported by F. Hoffmann–La Roche