Fully Automated Multi-Step Synthesis of Block Copolymers

An automated synthesis protocol is developed for the synthesis of block copolymers in a multi-step approach in a fully automated manner. For this purpose, an automated dialysis setup is combined with robot-based synthesis protocols. Consequently, several block copolymerizations are executed completely automated and compared to the respective manual synthesis. As a result, this study opens up the field of autonomous multi-step reactions without any human interactions.

A Reliable Automated Synthesis of 6-[18F]Fluoro-L-DOPA and the Clinical Application on the Imaging of Congenital Hyperinsulinism of Infants

6-[18F]fluoro-L-DOPA is a radiotracer widely used in the diagnosis of a range of diseases, including neuro-oncology, endocrinology, and Parkinson’s disease. To meet the fast growing clinical need for this radioactive compound, this study reports an optimized radiosynthsis of this molecule, which proved to be highly reliable and compatible with different types of automated radiosynthesizers. Moreover, with 6-[18F]fluoro-L-DOPA, the PET/CT imaging of a total of 23 patients has been conducted, further demonstrating this radiotracer as a clinically valuable reagent to diagnose congenital hyperinsulinism (CHI) of infancy and, more importantly, localize the exact lesion on pancreas.

DEVELOPMENT OF OPTIONS OF TECHNOLOGICAL SCHEMES PROCESSING OF MAIN TYPES OF GRAIN RAW MATERIALS

The processes of processing of grain raw materials are quite common at food and processing enterprises in Ukraine. This is due to the significant volumes and wide variety of these raw materials, as well as a wide range of semi-finished products and finished products that are obtained from them. In particular, the country's enterprises process such types of grain crops as wheat, barley, rye, corn, oats, rice, sorghum, millet, chumiza, mogar, paiza, buckwheat (buckwheat family), mealy amaranth (amaranth family). Peas, beans, lentils, soybeans and other legumes are also grown in large volumes. All these raw materials come from different farms, in different conditions, in a wide range of varieties and quality, thus, even for the same type of grain raw materials such parameters as the shape and size of grains, their weight, moisture, glassiness, hardness, degree of damage and many others may differ significantly. Depending on the type of products obtained from grain raw materials (flour, cereals, malt, bran, starch, gluten, molasses, alcohol grains, vegetable oil, oilcakes, meal), the technologies for its preliminary processing may have significant differences. The purpose of this work is to develop a methodology for choosing a rational sequence for processing grain raw materials, taking into account the initial quality parameters, conditions of a specific production and criteria for the efficiency of working processes (productivity, energy intensity and quality of finished products). The article also provides options for technological schemes for the preliminary processing of the main types of dry grain raw materials. The proposed sequence for the development of these technological schemes can further serve as the basis for creating a computer program for automated synthesis and analysis of rational options for technological processes for processing dry grain raw materials.

Using Automated Synthesis to Understand the Role of Side Chains on Molecular Charge Transport

The development of next-generation organic electronic materials critically relies on understanding structure-function relationships in conjugated polymers. However, unlocking the full potential of organic materials requires access to their vast chemical space while efficiently managing the large synthetic workload to survey new materials. In this work, we use automated synthesis to prepare a library of conjugated oligomers with systematically varied side chain composition followed by single-molecule characterization of charge transport. Our results show that molecular junctions with long alkyl side chains exhibit a concentration-dependent bimodal conductance with an unexpectedly high conductance state that arises due to surface adsorption and backbone planarization, which is supported by a series of control experiments using asymmetric, planarized, and sterically hindered molecules. Density functional theory simulations and experiments using different anchors and alkoxy side chains highlight the role of side chain chemistry on charge transport. Overall, this work opens new avenues for using automated synthesis for the development and understanding of organic electronic materials.

Automated synthesis of mobile robots of arbitrary orientation in the technological space

The research is devoted to the solution to the development of a methodology for the synthesis of mobile robots of arbitrary orientation in the technological space with systems for holding mobile robots on the moving surface to compensate for the gravitational and technological load. Mobile robots, also known in international publications as Climber Robot, are a new modification of mobile robots. The creation of this type of robotics is dictated by the need to perform technological operations in such areas as monitoring industrial facilities, erection and dismantling of building structures, repair and preventive maintenance of their components, maintenance of high-rise buildings of urban utilities, forest and park woodlands, etc. The operation of mobile robots acquires particular relevance in the extreme conditions of manmade disasters, which are dangerous and even unacceptable for a person's stay. The paper proposes designs of mobile robots, which are based on new principles of their synthesis. In the performed studies, in addition to the latest patented designs of mobile robots, a strategy of active synthesis of a new class of mobile robots is proposed.

Study of the automated synthesis of the radiopharmaceutical fluoroestradiol-18F

Approximately 75% of breast cancer cells express estrogen receptor positive, being the second leading cause of cancer death among women worldwide with an incidence of 25% per year. 16α-[18F]-fluoro-17β-estradiol, FES-18F, is a radiopharmaceutical that binds to estrogen receptors enabling the acquisition of molecular images for non-invasive diagnosis of primary and metastatic breast cancer using PET-CT. The objective of this work was to study the synthesis of FES-18F in the GE TRACERlab® MXFDG module, using the chemical kit and the ABX® disposable cassette, and to determine the process yield and the analytical parameters to be used in the routine production of this radiopharmaceutical. Automated synthesis occurs in 75 minutes and includes percolation of [18F-] fluoride into an anion exchange cartridge, cartridge elution, 3-step azeotropic drying, labeling using precursor 3-methoxymethyl-16β,17β-epiestriol-O-cyclic sulfone (MMSE) and a hydrolysis step. Product purification is done in the module using solid phase extraction (SPE) cartridges. The radiochemical yield was reproductive, regardless of fluor-18 activity at entry into the module, and the results of quality control tests suggest that the radiopharmaceutical meets the criteria established for other fluor-18-labelled radiopharmaceuticals that have monographs in official compendiums. In vivo biodistribution studies in healthy animals and with a tumor model developed with MCF-7 cells, demonstrated radiopharmaceutical uptake in excretory organs and specificity for breast tumor cells.

Production of 6-l-[18F]Fluoro-m-tyrosine in an Automated Synthesis Module for 11C-Labeling

6-l-[18F]Fluoro-m-tyrosine (6-l-[18F]FMT) represents a valuable alternative to 6-l-[18F]FDOPA which is conventionally used for the diagnosis and staging of Parkinson’s disease. However, clinical applications of 6-l-[18F]FMT have been limited by the paucity of practical production methods for its automated production. Herein we describe the practical preparation of 6-l-[18F]FMT using alcohol-enhanced Cu-mediated radiofluorination of Bpin-substituted chiral Ni(II) complex in the presence of non-basic Bu4ONTf using a volatile iPrOH/MeCN mixture as reaction solvent. A simple and fast radiolabeling procedure afforded the tracer in 20.0 ± 3.0% activity yield within 70 min. The developed method was directly implemented onto a modified TracerLab FX C Pro platform originally designed for 11C-labeling. This method enables an uncomplicated switch between 11C- and 18F-labeling. The simplicity of the developed procedure enables its easy adaptation to other commercially available remote-controlled synthesis units and paves the way for a widespread application of 6-l-[18F]FMT in the clinic.