Institute of organic chemistry National academy of sciences of Ukraine

 


   BIOLOGICALLY ACTIVE COMPOUNDS DEPARTMENT

The Department was founded in 1958 by Prof. P.S.Pelkis. Since 1980 the Department is chaired by Academician of the NAS of Ukraine M.O.Lozinskii. The staff of the Department is as follows: 2 Doctors of Science, 11 PhDs, 3 engineers.
The priority direction of the investigations is molecular design of the compounds, containing potentially pharmakophoric groups. The aim of the Department is to synthesize new functionalized N-, O-, S- and P-containing compounds on the base of classical methods and to elaborate original reagents and reactions, in particular new approaches to heterocyclizations and recyclizations. The main practical achievements of the Department are new medicinal preparations (Ademol, Amben, Mebifon, Nikorandil, Tomerzol, Yakton) created in the frames of the joint projects with the Institutes of the NAS of Ukraine (Bio-Chemistry, Food Bio-Technology and Genomics, Cell Biology and Genetic Engineering) and AMS of Ukraine (Pharmacology and Toxicology, Experimental and Applied Oncology and Radiology). Multi-purpose reagents 2-phenacyl-1H-benzimidazoles have been synthesized and introduced to the practice of organic synthesis. That allowed to elaborate methodology of new benzimidazole compounds obtaining and also pyrazole (by recyclization of benzimidazole cycle). There have been found and studied nine reactions which don’t have close analogs in literature.
5-Benzoyl-3-ethoxycarbonyl-6-methylthio-1,2-dihydropyridine-2-ones have been synthesized for the first time, it was shown that they react regio-selectively with heterocyclic nitrogen-containing 1,3-dinucleophiles forming condensed polycyclic heterosystems, including new ones: pyrido[2,3-d]­[1,2,4]triazolo­[1,5-a]pyrimidines, ­pyrazolo[1,5-a]pyrido[2,3-d] pyrimidines, pyrido­[2,3-d]pyrido­[2?,3?:3,4]­pyrazolo­[1,5-a]pyrimidines, 5Í-pyrido­[2,3-d]­thiazolo­[3,2-a]­pyrimidines and benzo­[4,5]imidazo­[1,2-à]­pyrido­[2,3-d]pyrimidines.
Convenient and preparative effective methods for the synthesis of unknown heterocyclic derivatives of (amino)bisphosphonates have been elaborated.
Since 2005 the Department has started investigation of the synthesis methods and heterocyclizations of  î-carboxibenzaldehydes and their structural analogs.


The Patent of Ukraine  ¹ 3177. 1-Adamantylethoxy-3-morpholino-2-propanol hydrochloride with utero-stimulating activity. – M.O.Lozinskii, Yu.B.Korotkii, I.I.Krasavtsev, L.M.Zaitsev, B.M.Klebanov, N.R.Gorodetskove – 1991.
 
Dzvinchuk I.B., Lozinskii M.O., 1-Arylmethyl-1Í-benzimidazoles and 2-Phenacylbenzthiazole in the Synthesis of Heterocyclic Compounds. Nitrogen-ContainingHeterocycles. Moscow, ICSPF PRESS, 2006. – Ò. 1. – Ñ. 275-287.
BritsunV.N., EsipenkoA.N., ChernegaA.N., RusanovE.B., LozinskiiM.O. – Synthesisand Transfromations of 3- benzoyl-6-oxo-5-ethoxycarbonyl-1-R-1,2,3,6-tetrahydropyridine-2-thiones // CHC. – 2007.- ¹11. - P.1660-1669.
Chuiko O.L., Filonenko L.P., Borisevich A.M., Lozinskii M.O. Synthesis Methods for Geminate Bisphosphonic Acids. // Ukr.Chem.J. . – 2002. – V. 68. – ¹ 11. –P. 9-17
Shelyakin V.V., Lozinskii M.O., Kartsev V.G.  o-Carboxybenzaldehydes and their Derivatives in the Synthesis of Isoquinoline Series Alkaloids// Selected Methods for the Synthesis and Modification of Heterocycles. Isoquinolines: Chemistry and Biological Activity Moscow, ICSPF PRESS ,2008 – V. 7. –P. 313-339.

   

   

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