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Information × Registration Number 0225U000726, (0120U100153) , R & D reports Title Development of new ways of obtaining substituted benzothiazoles, benzoxazoles, oxazolopyridines, thiazolopyridines, imidazopyrimidines and modification of their structures by transformation of functional groups popup.stage_title Розробка нових шляхів отримання та функціоналізація ізомерних імідазопіримідинів Head Tolkunov Sergej V., Доктор хімічних наук Registration Date 17-01-2025 Organization Institute of Physical and Organic Chemistry and Coal Chemistry. LM Litvinenko of the National Academy of Sciences of Ukraine popup.description1 To develop the methods for synthesis of heterocyclic derivatives of benzothiazoles, benzoxazoles, oxazolopyridines and thiazolopyridines, and to modify their structures by converting functional groups for searching of new biologically active compounds popup.description2  As a result of the performed research, a convenient way of synthesis of imidazo[1,5-a]pyrimidines by cyclization of in situ obtained 5-aminoimidazoles with various malondialdehydes or 1,3-diketones was developed. The synthetic limits of this reaction depending on the reagents and reaction conditions were studied, which makes it possible to widely vary the substituents in the pyrimidine cycle. A new C-N/C-C rearrangement of imidazo[1,5-a]pyrimidine into 3H-imidazo[4,5-b]pyridine core, which occurs in an acidic medium, was revealed. A probable mechanism of rearrangement is proposed. Counter synthesis of the obtained compounds was carried out. The carbonylation of 6-bromoimidazo[1,2-a]pyrimidine and 6-bromoimidazo[4,5-b]pyridine with carbon monoxide in the presence of [1,1'-bis(diphenylphosphino)ferrocene]dichloropalladium (Pd(dppf)Cl2), which led to the synthesis of methyl imidazo[1,2-a] pyrimidine-6-carboxylate and methyl imidazo[4,5-b]pyridine-6-carboxylate. A large array of imidazo[1,5-a]pyrimidines and imidazo[1,2-a]pyrimidines containing carboxylic acid substituents in various positions of imidazo[1,5-a]pyrimidines and imidazo[1,2-a] was synthesized pyrimidines and which can be used to create new drugs. Product Description popup.authors Bohza Serhii L. Lavrynenko Andrii A. Savytskyi Pavlo V. Smyrnova Olha V. Tolkunov Andrii S. Tolkunov Valerii S. popup.nrat_date 2025-01-17 Close
R & D report
Head: Tolkunov Sergej V.. Development of new ways of obtaining substituted benzothiazoles, benzoxazoles, oxazolopyridines, thiazolopyridines, imidazopyrimidines and modification of their structures by transformation of functional groups. (popup.stage: Розробка нових шляхів отримання та функціоналізація ізомерних імідазопіримідинів). Institute of Physical and Organic Chemistry and Coal Chemistry. LM Litvinenko of the National Academy of Sciences of Ukraine. № 0225U000726
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Updated: 2026-03-27