Vol. 23 No. 3 (2025)

The host-guest complexation of cone-shaped calix[4]arene-hydroxymethylphosphonic acid (CPA) and calix[4]arene-hydroxymethyldimethylphosphine oxide (CPO) with active pharmaceutical ingredients of antiviral drugs Remdesivir, Nevirapine, Vesatolimod, and Bictegravir in the aqueous-organic mobile phase on a Zorbax CN column has been studied using RP HPLC method. By analyzing the dependence of the drug capacity values on the concentration of calixarene in the mobile phase, the stability constants (К_А = 3672 - 6884 M^-1) of the complexes formed have been determined. Quantum-chemical calculations show that the drugs studied form supramolecular exo-complexes with CPA and CPO molecules. These complexes are stabilized by intermolecular hydrogen bonds of proton donor groups P(O)(OH)₂ CPA and proton acceptor groups Me₂P=O CPO with the amino group of Remdesivir, the amide group of Nevirapine, the amino group and amide group of Vesatolimod, and the amide group of Bictegravir.

In this study, an optimized method for the synthesis of azaindoles was developed and successfully scaled up to a 100 g batch. Improved yields were observed when using electron-deficient azaheterocycles and substrates bearing electron-withdrawing substituents. 6-Chloro-1H-pyrrolo[3,2-c]pyridine was selected for further functionalization using a carbonylation protocol involving carbon monoxide. As a result, novel and promising building blocks for medicinal chemistry were obtained.

The interaction of enantiomerically pure N-tert-butylsulfinyl imines of trifluoropyruvate with diazomethane has been studied. It has been shown that there is the [3+2]-cycloaddition at the initial step with the formation of diastereomeric trifluoromethyltriazoline carboxylates in the ratio of 5.6:1. Treating the triazoline carboxylates with trifluoroacetic acid yielded optically pure aziridine carboxylates, which were subsequently converted into their corresponding acids. When subjected to hydrochloric acid in an ethereal solution, trifluoromethylaziridines underwent ring-opening and the sulfinyl group removal, producing α-chloromethylamino acids. The study also demonstrates the potential use of these aziridinecarboxylic acids in the peptide synthesis.

The aim of the article is to present the results of the experimental study of leachables used as primary packaging for medical devices, namely injectable implants based on hyaluronic acid. For the study, a line of injectable implants with identical qualitative composition and differing quantitative hyaluronic acid content was used. When developing the research conditions, the main characteristics of the implant gel were taken into account, and the conditions for using the appropriate medical device were modeled to obtain the most informative results and confirm the safety of the primary packaging selected. The analysis of extracts was carried out using the following methods: GC/MS, HPLC/UV/MS, ICP/MS, and IC. No substances listed as Chemicals of Potential Concern were detected in the extracts obtained, thereby confirming the safety of using the medical device for the patient under the conditions specified by the manufacturer.

A one-pot, stepwise method for the annelation of the 1,2,4-triazine core to the seven-membered 2,3-benzodiazepine ring via the interaction of the corresponding 2,3-benzodiazepin-1-yl- or 2,3-benzodiazepin-4-ylhydrazines with α-ketoesters has been developed. It has been found that a stepwise formation of an azomethine intermediate followed by solvent replacement and subsequent cyclization enables the desired compounds to be obtained in high yields. Derivatives of a new heterocyclic system of [1,2,4]triazino[3,4-a][2,3]benzodiazepine have been synthesized.

The Ukrainian school of organic dye chemistry has long received worldwide recognition. Among the scientists whose achievements embody this success is Academician Oleksandr Oleksandrovych Ishchenko. Over more than half a century of fruitful research at the Department of Color and Structure of Organic Compounds of the Institute of Organic Chemistry of the National Academy of Sciences of Ukraine, he laid the foundations for the rational design of functional dyes for light-energy conversion, particularly for various laser technologies; became one of the pioneers of polymethine ion-pair photonics; developed methodological approaches to the study of electronic absorption and fluorescence spectra using the method of moments, which provided new insights into the electronic structure of organic chromophores; and made a significant contribution to the systematic study and interpretation of the solvatochromism of polymethines of different types. The driving force behind all these achievements was his enduring passion for science — a deep desire to learn and share knowledge with future generations of researchers.