Targeted Synthesis of 3,3′-, 3,4′- and 3,6′-Phenylpropanoid Sucrose Esters

In this study, we report on an orthogonal strategy for the precise synthesis of 3,3′-, 3,4′-, and 3,6′-phenylpropanoid sucrose esters (PSEs). The strategy relies on carefully selected protecting groups and deprotecting agents, taking into consideration the reactivity of the four free hydroxyl groups of the key starting material: di-isopropylidene sucrose 2. The synthetic strategy is general, and potentially applies to the preparation of many natural and unnatural PSEs, especially those substituted at 3-, 3′-, 4′- and 6′-positions of PSEs.

Diastereoselective Indole-Dearomative Cope Rearrangements by Compounding Minor Driving Forces.

Reported herein is the discovery of a diastereoselective indole-dearomative Cope rearrangement. A suite of minor driving forces (substrate destabilizing effects; product stabilizing effects) are what promote this otherwise unfavorable dearomatization reaction. These include the following that work in concert to overcome the penalty for dearomatization: (i.) steric congestion in the starting material, (ii.) alkylidene malononitrile and stilbene conjugation events in the product, and (iii.) an unexpected intramolecular p–p* stack on the product side of the equilibrium. The key substrates are rapidly assembled from alkylidenemalononitriles and indole-phenylmethanol derivatives resulting in many successful examples (high yields and diastereoselectivity). The products are structurally complex bearing vicinal stereocenters generated by the dearomative Cope rearrangement. They also contain a variety of functional groups for interconversion to complex architectures. On this line, also described herein are proof-of-concept strategies for achieving enantioselectivity and conversion of the dearomative products to valuable and functionalized small drug-like molecules.

The influence of annealing conditions on Ca/P ratio and phase transformations in bulk calcium phosphates

The present study investigates the influence of annealing conditions on phase transformations in calcium phosphates. Synthetic brushite (CaHPO4∙2H2O) with Ca/P ratio 1:1 was taken as a starting material and annealed...

15 Paired Electrolysis

While paired electrochemical reactions have a history that can be traced back to the 19th century and have been very effectively used for the production of commercial products, the larger synthetic community has only recently started to embrace the opportunities this approach offers to maximize the overall energy and atom efficiency of electrochemical processes. In this review, a summary of these efforts is presented in the context of four classes of paired electrochemical reactions. These classes of reaction involve parallel processing of products at the anode and cathode, divergent reactions that use a single starting material in different ways, convergent reactions that combine products made at the anode and cathode, and sequential reactions that pass a substrate between the electrodes.

Particle Characterisation of Traditional Homeopathically Manufactured Medicine Cuprum metallicum and Controls

Background: Homeopathy is highly controversial. The main reason for this is its use of very highly dilute medicines (high homeopathic potencies, HHP), diluted beyond the Avogadro/Loschmidt limit. Research using several different methods has demonstrated the presence of particles, including nanoparticles of source material, in HHPs. This study aims to verify the results of a previous publication that detected the presence of particles in all dilutions. Methods: We used the Nano Tracking Analyzer (NTA) to examine dilutions of a commonly used homeopathic medicine, an insoluble metal, Cuprum metallicum, for the presence of particles. The homeopathic medicines tested were specially prepared according to the European pharmacopoeia standards. We compared the homeopathic dilutions/dynamizations with simple dilutions and controls including a soluble medicine. Results: We observed the presence of solid material in all preparations including HHPs (except for pure water). The measurements showed significant differences in particle sizes distribution between homeopathic manufacturing lines and controls. Conclusion: Homeopathic medicines do contain material with a specific size distribution even in HHPs diluted beyond the Avogadro/Loschmidt limit. This specificity can be attributed to the manufacturing and potentization process. This material demonstrates that the step-by-step process (dynamized or not) does not match the theoretical expectations in a dilution process. The starting material and dilution/dynamization method influences the nature and concentration of these NPs.

Identification and Semisynthesis of (–)-Anisomelic Acid as an Oral Antiviral Agent against SARS-CoV-2 in Mice

(–)-Anisomelic acid (AA), isolated from Anisomeles indica (L.) Kuntze (Labiatae) leaves, is a macrocyclic cembranolide with a trans-fused α-methylene-β-lactone motif. Cytopathic effect assays showed that the anti-SARS-CoV-2 effect of AA (IC50 = 4.3 μM) is comparable to that of remdesivir (IC50 = 2.1 μM), and more potent than that of molnupiravir (IC50 = 27.8 μM). Challenge studies in SARS-CoV-2-infected K18-hACE2 mice showed that oral administration of AA and remdesivir can both reduce the viral titers in the lung tissue at the same level. To facilitate drug discovery, we used a semisynthetic approach to shorten the project timelines. The enantioselective semisynthesis of AA from the naturally enriched and commercially available starting material (+)-costunolide was achieved in five steps with a 27% overall yield. The developed chemistry provides opportunities for developing AA-based novel ligands for selectively targeting proteins involved in viral infection.

Productivity and quality of fiber’s varieties and selection numbers of flax in the Urals of the nonblack earth zone of Russia

In the Ural of the nonblack earth zone of Russia, fiber flax variety Diane from France and selection number ER-138 from Russia stood out in fiber yield. One of the parameters for obtaining a homogeneous fiber of fiber flax is the technical length of the stem - not less than 60 cm, the thickness of the stem - not less than 500 units. The selection number K4196 × 1288/12 and the variety TOST 4 from Russia, which were characterized by a high technical length (61.2 - 61.8 cm) and dryness (472 - 509 units) of the stem in all the years of study in relation to the standard grade. The indicated breeding numbers and varieties, distinguished by yield, technical length and stem thickness, can serve as a starting material in the breeding process. Keywords: FIBER FLAX, VARIETY, BREEDING NUMBER, YIELD, FIBER, TECHNICAL LENGTH, MYKLOST

New Derivatives of Lupeol and Their Biological Activity

The natural product lupeol (1) was isolated from Bombax ceiba leaves, which were used as starting material in the semisynthetic approach. Three new derivatives (2a, 2b, and 3) were synthesized using oxidation and aldolization. Their chemical structures were elucidated by spectroscopic analyses (HRESIMS and NMR). Compounds 3 showed significant α-glucosidase inhibition with an IC50 value of 202 µM, whereas 2a and 2b were inactive.

Protein content in grain of collection samples of common pea and its adaptive properties

The purpose of the research was to identify samples of the collection of peas with a high and stable protein content in the grain, as a starting material in breeding for grain quality. Of the 130 studied samples of the collection of peas, which had at least 25.0% of the protein content in the grain, on average over the years of research, only 13 samples had a protein content of at least 25.0%. The highest minimum protein content was observed in the Russian-bred OMK-3 sample, which had an indicator of 26.1%. For the rest, the minimum value was from 25.0 to 25.3%. The maximum protein content over the years of research in pea samples was from 25.8 to 29.7%, of which samples 193/73 (Ukraine) (29.7%), OMK-3 (Russia) (29.5%), NS-01-68 (Bulgaria) (29.1%), B-887 (Russia) (28.7%) and Orel-330 (Russia) (28.7%). The average value of the coefficient of variation for varieties, characterizing intravarietal variability, was 6.8% on average for the collection, with the lowest value being 1.2% and the highest value being 15.9%. In the 13 isolated samples, the intravarietal variability was lower than the average for the collection as a whole (1.2-6.6%), except for sample 193/73 (Russia), for which it was 7.3%. This sample has the highest average and maximum protein content in the years of research. The selected 13 samples from the pea collection are of breeding value as initial parental forms in the direction of increasing the protein content in the pea grain and enhancing the stability of this indicator.

Environment Influence on the Properties of Functional Parts Made of HIPS Material

The aim of this work is to study the climatic influences on 3D printed materials. This study focuses on the HIPS material, which was chosen as the starting material for further studies. The material in the field of 3D printing is known for its rapid photooxidation, which results in the formation of cracks in the final product. A climatic chamber was used for degradation, in which UV light, heat and increased humidity were applied to the material. The degree of degradation was then checked by tensile test and electron microscope.