Announcement about the defense of the doctoral (DSc) thesis of Abdurazakov Askar Sheraliyevich

Thesis defense will be on September 20, 2023 at 10:00.

I. General information.

The topic of the dissertation, specialty code (the name of the branch where the academic degree is awarded): «Synthesis and technology of highly effective drugs in the series of benzimidazoles, quinolines and quinazolines for agriculture and medicine», 02.00.03 – Organic chemistry, 02.00.14- Technology of organic substances and materials based on them (technical sciences).

Dissertation topic registered number: В2022.2.DSc/T519.

Scientific advisors: Sagdullayev Shomansur Shokhsaidovich, doctor of technical sciences, professor. Elmuradov Burkhon Jurayevich, doctor of chemical sciences, professor.

Name of the institution where the dissertation was completed: Institute of the Chemistry of Plant Substances.

Name of the institution where the scientific council works, Number of the scientific council: Institute of the Chemistry of Plant Substances, DSc.02/30.01.2020.K/T.104.01.

Official opponents: Abdushukurov Anvar Kabirovich, doctor of chemical sciences, professor; Vapoev Khusnitdin Mirzoyevich, doctor of technical sciences; Khalilov Ravshanjon Muradjonovich, doctor of technical sciences.

 

Leading organization: Tashkent institute of chemical technology

Dissertation direction: theoretical and practical.

 

II. The aim of the study to develop of methods for the synthesis of new derivatives of benzimidazole, quinoline, bi-, tricyclic quinazolines, study of their structure, physicochemical and biological activity, development of technology for the industrial production of highly active compounds and improvement of existing technologies.

III. The scientific novelty of the dissertation research is as follows:

directed synthesis and modification of benzimidazole, quinoline, quinazoline and their derivatives were studied, 78 compounds were synthesized and their structure was confirmed by modern physical research methods;

for the first time, the structure of the Alpec preparation obtained from albendazole and pectin as a “polymer complex” was reliably proven on the basis of physicochemical research methods (potentiometric titration, X-ray phase analysis, IR spectroscopy);

for the first time, the acylation reactions of 2-BMC isolated from local raw materials - waste products of medamin preparation with carboxylic acids were carried out with practical significance and the main factors affecting the course of the reaction (substrate structure, acid nature, temperature and reaction time) were determined and a possible reaction mechanism was recommended;

for the first time, a water-soluble stable preparative form of the herbicidal composition Mefosin based on 2-methyl-5-chlorobenzimidazole hydrochloride and glyphosate was recommended for practical use;

the reaction of obtaining difficult-to-synthesize 6-aminoquinazolin-4-one was successfully carried out and an alternative and effective method for its acylation with cheap carboxylic acids was proposed, and the main factors affecting the yield of products were identified;

The condensation of tricyclic quinazolone alkaloids and their substituted derivatives with various aromatic aldehydes in the presence of acidic catalysts has been systematically studied and it has been established that the reactions proceed with the participation of activated methylene groups and the formation of arylidene derivatives in the E-isomer form, the factors affecting the course of reactions and the yield of products have been determined, reaction mechanism recommended;

Gel, powder and tablet forms of Alpec, stable suspension forms of 2.5%, 10% albendazole were obtained, the factors affecting the physical properties of these dosage forms were studied.

IV. Implementation of research results. Based on the obtained scientific results on the synthesis of new derivatives of benzimidazole, quinoline, quinazolone, determination of their structure, reactivity and biological properties, development and implementation of technology for obtaining modified forms of active substances:

received a patent for an invention (No. IAP06408, 2021) of the Intellectual Property Agency of the Republic of Uzbekistan for a method for producing an anti-echinococcosis agent (Alpec). As a result, a highly effective anthelmintic agent for use in medicine has been created;

received a patent for the invention of the Agency for Intellectual Property of the Republic of Uzbekistan for the non-selective herbicidal composition Mefosin (No. IAP05934, 2019). The result is a water-soluble, low-toxicity and highly effective herbicidal composition against weeds in non-agricultural areas;

approved technical specifications for the suspension of the drug Alsus (2.5%; 10%) (Ts 03535440: 028-2016) with anthelmintic activity, substances Acetamisole (Ts 03535440-32: 2019) and Quinazol (Ts 03535440-034: 2019) by "Agency for standardization, coordination of state control and introduction of information technologies”. As a result, it was possible to introduce new, economical technologies for the industrial production of Alsus, Acetamisole and Quinazol preparations into practice;

approved technological instructions for the production of the drug "Alsus" (TI 03535440-028:2017) by the "Main State Department of Veterinary Medicine under the Ministry of Agriculture and Water Resources of the Republic of Uzbekistan", for the production of substances Acetamisole (TI 03535440-32:2018) and "Quinazol" (TI 03535440-033:2019) by "The Main State Department for Quality Control and Circulation of Veterinary Medicines and Food Additives of the Republic of Uzbekistan". As a result, cost-effective technologies for the industrial production of substances Alsus, Acetamisole and Quinazol made it possible to put into practice;

VFS 42 Uz-3069-2017 for the substance and VFS 42 Uz-3070-2017 for the tablet form of Nitroxoline are approved by the “State Center for Expertise and Standardization of Medicines, Medical Devices and Medical Equipment of the Ministry of Health of the Republic of Uzbekistan”. As a result, this made it possible to introduce a new cost-effective industrial technology for the production of Nitroxoline;

X-ray diffraction analysis of 2-amino-1H-benzimidazol-1-yl)(phenyl)methanone is included in the Cambridge Central Crystallographic Database, https://www.ccdc.cam, CCDC 2049631. As a result, the introduction of a new compound into the database made it possible to determine the structure of similar substances.

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