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Information × Registration Number 0221U106698, 0116U008794 , R & D reports Title The minimalist design of synthetic routes in the synthesis of azoloazines, azolo(azino)dіazepines and other polyannelated heterocyclic systems popup.stage_title Head Bogza Serhii Leonidovych, д.х.н. Registration Date 17-12-2021 Organization Institute of Organic Chemistry NAS of Ukraine popup.description2 Heterocyclic analogues of isoquinoline and benzodiazepines are little studied classes. The formation of a fused pyridine or 1,2-diazepine ring requires the organization of a five-carbon chain with active terminal fragments on the heterocyclic nucleus. The solution is to modify the classical reactions by using multifunctional reagents with controlled reactivity to obtain products directly suitable for the next synthetic stages. Reactions that are able to form functionalized intermediate heterocyclic products in one or two cycles. New good methods have been developed and the reactivity of 4-S-oxoalkylsulfides of 2,3-benzodiazepines, which can be used as building blocks for bioactive compounds, has been studied. Their transformation under the conditions of the sulfide compression reaction was studied, which made it possible for the first time to obtain ketones and acids of the 2,3-benzodiazepine series. The annealing of the thiophene cycle to the seven-membered ring of 2,3-benzodiazepine has been developed. An effective method for the synthesis of pyrazolo [3,4-c] [2] benzazepines and 2,3-benzodiazepine derivatives condensed with the pyrimidine nucleus has been developed. It was found that 2-aminoindolizines with halomethyl ketones form [1,4] thiazepino [5,6-b] indolizin-5-imines, derivatives of the new heterocyclic system. The thiazepine cycle compression reaction was found. New original preparative methods for the synthesis of nonclassical Picte-Spengler reaction substrates have been developed, and their heterocyclizations have been studied. An effective approach to spiro-coupled pyrazolo [3,4 ‑ c] isoquinolines has been proposed. Their regrouping was found in the system, which leads to the destruction of the spiro system. A convenient method for obtaining 4-cyanocarbolines and pyrazolo [3 ', 4': 5,6] pyrido [3,4-b] indole has been developed. Among the synthesized compounds with high activity against the causative agent of leishmaniasis and anticancer were found Product Description popup.authors Bohdan Natalia M Stepanova Diana S Khairulin Andrii R Shuvakin Serhii I Yakovleva Hanna V popup.nrat_date 2021-12-17 Close