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High-selective methods of synthesis of heterocyclic compounds, components of functional materials and creation of novel medicines

Work number - P 18 AWARDED

Submitted by State Scientific Institution “Institute for single crystals” of NAS of Ukraine

Authors: Brovarets V.S., Vovk M.V., Desenko S.M., Lesyk R.B., Lipson V.V., Lyapunov M.O., Obushak M.D., Chebanov V.A.

The main aim of the work is creation and development of modern high-selective methods for construction of structurally diverse heterocyclic systems – bioactive substances and components of novel functional materials, as well as development of medicines in different forms.

In the work it was carried out the comprehensive research on key stages of creation of novel medicines and other functional materials, in particular:development of potentialities of organic chemistry focused at the search of new organic reactions and novel synthetic methods, convenient and easily available reagents and catalysts; analysis of structure-property correlations; routes of directed design of drug-like molecules; development of components and technologies of medicines.

Novel synthetic approaches to the creation of new types of nitrogen- and sulfur-containing five-, six-, and seven-membered heterocyclic systems with high synthetic, pharmacological, photoactive, chelating and agrochemical potential have been proposed, as well as the existing synthetic approaches have been markedly improved. The principles of controlled high-selective organic synthesis of structurally diverse heterocycles and heterocyclic ensembles have been elaborated. A number of principle concepts of organic chemistry related to the structure, reactivity and problem related to the directed functionalization of organic compounds have been developed.

The practical importance of the work lies in concrete achievements in the frame of concept «from molecule to medicine and novel functional materials», which includes development and application of novel synthetic methods for obtaining bioactive substances, components of materials with wide range of functional properties, original heterocyclic compounds and new heterocyclic systems, novel reagents and catalysts for fine organic synthesis, as well as creation of medicines.

The preparatory synthetic procedures for the series of azoles and azines “building blocks”, as well as their fused and hydrogenated derivatives have been elaborated. More than 300 systematic heterocyclic series have been synthesized (more than 100 thousands of new organic compounds have been obtained in total), the biological activities of sufficient amount of the compounds obtained were discovered and candidates to medicines were identified.

The rules of standardization of pharmaceutical products of Ministry of Health of Ukraine and 24 normative documents regulating circulation of drugs have been created. A range of 75 medicines has been developed, registered and implemented into production. The volume of sales of these drugs in the Ukrainian market (2008-2017) amounted to 123.67 million packages in the total amount of 3.41 billion UAH.

The results of the work have been presented in 51 monographs, 873 articles and 27 normative documents of the Ministry of Health of Ukraine; 159 patents have been obtained. All the publications included into the work have hindex (Scopus) of 34, and citation index of 5601. The results of the researches related to the topic have been included into 15 doctoral and 96 PhD theses. The number of implementations of the results of work, which are confirmed by the relevant acts, is 27.