Registration Number
0224U000706,
0121U100387
, R & D reports
Title
Design and development of strategies for the synthesis of boron and sulfur-organic building blocks, focused on the search for new drugs.
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Head
Hryhorenko Oleksandr О., Доктор хімічних наук
Registration Date
11-01-2024
Organization
Taras Shevchenko National University of Kyiv
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Object of research – saturated fused, bridged, spirocyclic and heterocyclic building blocks based on sulfonylfluorides, sultams, sulfoximines, as well as fluorinated bifunctional derivatives and aminoacids.
Aim of work – design and development of approaches to the synthesis of novel building blocks for drug discovery, in particular, sulfonylfluorides, sultams, and sulfoximines based on saturated fused, bridged, spirocyclic and heterocyclic systems.
Methods of research – methods of target-oriented (TOS), diversity-oriented (DOS), lead-oriented (LOS) synthesis for constructing novel building blocks –sulfonylfluorides, sultams, and sulfoximines; methods of high-pressure synthesis, synthesis under inert
atmosphere and irradiation; NMR spectroscopy, chromatomass-spectrometry, elemental analysis and X-Ray diffraction studies, acid-base titration.
Methods have been developed for the synthesis of novel building blocks derived from [3+2] cycloaddition reactions involving alkenyl boronates. Additionally, mono- and difluorinated saturated heterocyclic amines and fluoroalkyl-substituted cyclobutanes have been successfully synthesized using these methodologies. The exploration of Levin's "Nitrogen Removal" reaction has been demonstrated as a promising avenue for expanding the chemical space of sp3-enriched compounds. A comprehensive investigation into the physicochemical properties of the synthesized compounds has been undertaken, revealing key correlations between their structural features and properties. These correlations are of significant relevance in the context of medicinal chemistry, providing insights into the structural determinants that play a decisive role in governing the properties of these compounds.
Product Description
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Vashchenko Bohdan V.
Hryschuk Oleksandr V.
Lyashuk Oleksandr S.
Melnykov Kostyantyn P.
Chernykh Anton V.
Yurov Yevhen Yu.
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2024-01-11
