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Information × Registration Number 0223U004832, 0123U102747 , R & D reports Title Development of novel anesthetic agents popup.stage_title Head Mykhailiuk Pavlo K., Доктор хімічних наук Registration Date 05-12-2023 Organization Taras Shevchenko National University of Kyiv popup.description2  Research object: bioisosteres of piperidine, amino acids, spirocycles. The purpose of the work: development of synthetic approaches to new cyclic amino acids – analogues of pipecolic acid and their synthesis. Research methods: literature analysis, test reactions, scaling of synthesis methods,1H, 13C NMR spectroscopy, mass spectrometry, chromatography. Based on the analysis of the literature, the most probable ways of synthesis of new cyclic amino acids were chosen. After experimental verification on test reactions in small quantities, a strategy for the approach to the creation of new 3D Fsp3-enriched bioisosteres of piperidine - analogs of pipecolic acid - was formed for the first time. This strategy made it possible to remove synthetic restrictions on the use of the 1-azaspiro[3.3]heptane fragment and introduce it into the composition of new amino acids, which are biologically confirmed bioisosteres of the new generation of piperidine. The obtained test results were analyzed, the influence of various factors (catalyst, temperature, solvent, steric factors, electronic factors, etc.) on the course of reactions was evaluated. The influence of competitive reactions, the possibility of rearrangement, the dependence of the structure of products on the ratio of reagents are taken into account. Based on this, the ways of synthesis of new cyclic amino acids were adjusted and optimal conditions were found. Product Description popup.authors Yehorova Tetyana V. Kyrychok Oleksandr O. popup.nrat_date 2023-12-05 Close