PhD thesis has been defended

The defense of the PhD thesis titled "Reactions of α-aminoazoles with 4-oxobenz[1,3-e]oxazimium perchlorates and three-component condensations with cyclic CH-acids and glyoxals in the synthesis of azoloazines" by Petrova O.M., the junior research scientist of SSI STC "Institute for Single Crystals", has been held on June 04, 2015.

Thesis for PhD degree in Chemistry, specialty 02.00.03 – organic chemistry. State higher educational establishment Ukrainian State University of Chemical Technology, Dnipropetrovsk, 2015.

The present thesis is devoted to the investigation of the direction of 3(5)-amino-pyrazole, 3-amino-1,2,4-triazole, and 2-aminobenzimidazole with 4-oxobenz[1,3-e]-oxazimium perchlorates interaction, and also their thee-component condensation with glyoxal or arylglyoxas hydrates and cyclic β-dicarbonyl compounds, such as 2,2-dimethyl-1,3-dioxane-4,6-dione, cyclohexane-1,3-dione and indan-1,3-dione. Methods for the synthesis of pyrazolo[3,4-d]pyridine, pyrazolo-, triazolo[1,5-a][1,3,5]triazine, partially hydrogenated 4-aroyl substituted pyrazolo[3,4-b]pyridin-6-one, -[3,4-b]quinolin-5-one, 5-aroyl-6-oxopyrazolo[1,5-а]quinoline, indolo[1,2-с]azolo[1,5-а]quinazolin-8,10-dione and 4-aroylindeno[1,2-b]pyrazolo[4,3-e]pyridin-5(2H)-one derivatives are proposed. It is shown that all synthetic methods are based on high selective domino-reactions. Special attention is given to the new pseudo four-component regioselective cyclocondensation of cyclohexane-1,3-dione, monocyclic α-aminoazoles and glyoxal hydrate. This condensation leads to the formation of new indolo[1,2-с]azolo[1,5-а]quinazolin-8,10-dione heterocyclic system. Chemical transformations of synthesized compounds are presented. The results of virtual screening (by the docking method) on the target for antidiabetic drugs 11β-HSD1 are discussed.

Keywords: α-aminoazoles, 4-oxobenz[1,3-e]oxazimium perchlorates, glyoxal hydrate, arylglyoxales, cyclic СН-acids, azoloazines, domino-reactions, regioselectivity.

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