Registration Number
0213U001633,
0112U008268
, R & D reports
Title
Mulicomponent cascade regioselective and stereoselective synthesis of new organic compounds, partially saturated O-,S, Se-containing azaheterocycles, and study their biological activity
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Head
Krivokolysko Sergii Gennadievich,
Registration Date
16-01-2013
Organization
EAST-UKRAINIAN VOLODIMIR DAL NATIONAL UNIVERSITY
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A new perspective direction in heterocyclic chemistry is based on the aminomethylation of accessible substrates. The structures of new compounds were determined by means of modern analytic methods, reactions of the obtained compounds were studied. Regularities in the reaction of cyanothioacetamide with aliphatic/aromatic/cinnamic aldehyde, formaldehyde and primary amines were studied. We have developed a brand new cascade approach to thiazolo[3,2-a]pyridine based on the reaction of N-methylmorpholinium 4-aryl-3-cyano-6-oxo-1,4,5,6-tetrahydropyridine-2-thiolates with isobutyraldehyde and primary amines. The regularities in the aminomethylation of 6-аmino-4-aryl-3,5-dicyanopyridine-2(1Н)-thiones were studied. A cascade approach to 3,5,7,11-tetraazatricyclo[7.3.1.02,7]tridec-2-ene-8-selenones have been developed. We have found a new approach to functionalized pyrimidines by cascade reaction of enamino 1,3-dicarbonyls with 3-amino-3-thioxopropaneamides (thiomalonamides). Polyheterocyclic ensembles were obtained by reaction of 8-chloromethyl-3-methyl-7-(2-oxo-2-phenylethyl)xanthines with 3-cyanopyridine-2(1Н)-thiones. We succeeded to obtain pyrido[3',2':4,5]thieno[3,2-d][1,3,2]diazaphosphorines by treatment of 3-aminothieno[2,3-b]pyridine-2-carboxamides with P4S10. The obtained results allowed us to obtain 1,3,5-(thia)selenadiazines, pyrido-1,3,5-triazines, dipyridotetrazocines, polycyclic structures etc. under one-pot cascade process conditions. New compounds were tested for antiviral activity, some of them were found to be highly active and then were selected as hits for further testing.
Product Description
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Абраменко Віктор Леонідович
Доценко Віктор Вікторович
Фролов Костянтин Олександрович
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2020-04-02