Registration Number
0219U000815,
0117U004137
, R & D reports
Title
Polyfunctional derivatives of 2-alkyl(alkolden)-2,3-deggrading-4(1H)-ones. Synthesis and properties
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Head
Yavolovskii A.A.,
Registration Date
27-02-2019
Organization
A.V. Bogatsky, Physico-Chemical Institute of the National Academy of Sciences of Ukraine
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Objects or research 2-(beta-oxoalkyl)-pyrimidine-4 (3H)-ones, activated imines (2-alpha-hydroxyiminoethylpyrimidines, 2-alpha-tosyloxyiminoethylpyrimidines). Aim of research development of methods for synthesis of polyfunctional pyrimidine derivatives with nitrogen, oxygen and Possibility of using 2-alkyl pyrimidin derivatives, containing an activated imino group in ?-position of side chain as electrophilic component in reactions of forming nitrogen-sulfur bonds, was investigated. As a result was found, that reaction of thiourea with derivatives of 2- (2-oxo-2 sulfur-containing functional groups, by modifying 2-alkyl (alkylidene) pyrimidines, containing active nucleophilic and electrophilic centers in exocyclic part of molecule.-phenyl-1- (1-tosyloxyimino) ethyl) -pyrimidin-4 (3H) -ones leads to the substitution of the p-toluenesulfonyl group to form (Z, E) -2- (1- (formamidinosulfenimino) -2-oxo-2-phenylethyl) pyrimidine-4 (3H) -one p-toluenesulfonates. It was found, that reaction of potassium rhodanide or potassium selenocyanate with 2- (2-oxo-2-phenyl-1- (1-tosyloxyimino) ethyl) -6-phenylpyrimidine-4 (3H) -ones has been found to form a new condensed heterocyclic system the nitrogen atom is 3-benzoyl-7H-1,2,5-thia (seleno) diazolo [2,3-a] pyrimidine-7-ones. Twelve polyfunctional 2-alkyl (alkylidene) pyrimidine derivatives were tested for antibacterial and antitumor activity; Among the studied compounds, a cytotoxic effect in concentrations of 5.96-18.71 mM / L was detected in 2- {2 - [(2-bromophenyl) hydrazono] 2-phenylethyl} -6-methyl-3H-pyrimidin-4-one.
Product Description
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Іванов Юрій Едуардович
Грищук Лідія Володимирівна
Плужник-Гладир Сергій Михайлович
Степанов Дмитро Євгенович
Яволовський Аркадій Олександрович
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2020-04-02
