IV International Conference СВС2010
"Modern Aspects of Chemistry of Heterocycles"
dedicated to Prof. A.N. Kost's 95th birthday anniversary

was held at the Beloselsky-Belozersky Palace, Saint-Petersburg

August 2–6, 2010

 

This Conference continues the series of international meetings first held in 2001 on the Chemistry and Biological Activity of Synthetic and Natural Compounds.

 

The Conference was organized by the International Charitable Foundation Scientific Partnership
and InterBioScreen Ltd.
and with the participation and support from
Russian Academy of Natural Sciences, Russian Mendeleev Chemical Society, Moscow State University,
Saint-Petersburg State University, Saint-Petersburg State Institute of Technology (Technical University)
and Russian Academy of Sciences.

 

The Organizing Committee was headed by Prof. V.G. Kartsev, full member of the Russian Academy of Natural Sciences, President of the Scientific Partnership Foundation; Chairman of Board of Directors of InterBioScreen.

 

 

 

Honorary members of the International Editorial Board:

 

Prof. Corey E.J. (USA) – Nobel Prize in Chemistry, 1990

Prof. Noyori R. (Japan) – Nobel Prize in Chemistry, 2001

Prof. Lehn J.-M. (France) – Nobel Prize in Chemistry, 1987

Prof. Attanasi O.A. (Italy)

Prof. Atta-ur-Rahman (Pakistan)

Prof. Bergman J. (Sweden)

Prof. Elguero J. (Spain)

Prof. Huisgen R. (Germany)

Prof. Katritzky A.R. (USA)

Prof. Mąkosza M. (Poland)

Prof. van der Plas H. (the Netherlands)

Prof. Spinelli D. (Italy)

Prof. Stanovnik B. (Slovenia)

The scientific committee of the conference was composed of eminent Russian and CIS scientists in the field of chemistry and biological activity of synthetic and natural heterocycles:

 

 

Organizing Committee:

 

 

The composition of the conference covered a wide range of organic chemists working in the field of biologically active heterocyclic compounds. The Conference provided an opportunity for researchers to present their latest developments on the synthesis and chemical transformations, as well as the biological activity of heterocyclic compounds, covering a large variety of heterocycles from simple to complex condensed systems, synthetic and natural.

 

Among the participants were world-known representatives of the international heterocyclic community Prof. van der Plas H. (University of Wageningen, the Netherlands), Prof. Mąkosza M. (Institute of Organic Chemistry, Poland), Prof. Stanovnik B. (University of Ljubljana, Slovenia), Prof. Spagnolo P. (Università di Bologna, Italy), Prof. Yamamoto Y. (Tohoku University, Japan), Prof. Preobrazhenskaya M.N., Prof. Zefirov N.S., Prof. Chupakhin O.N., Prof. Pozharskii A.F., Prof. Brovarets V.S., Prof. Przheval'skii N.M.

 

 

Presidium of the conference

Prof. Spinelli D., Prof. Mąkosza M., Prof. van der Plas H., Prof. Preobrazhenskaya M.N., Member of Presidium of RANS Prof. Pototsky V.V., Prof. Stanovnik B., Prof. Zefirov N.S., Prof. Chupakhin O.N.

 

Contributions to the Conference were submitted by leading scientists of Austria, Belgium, Germany, Great Britain, Greece, Hungary, Egypt, India, France, Jordan, Italy, the Netherlands, Sweden, Russia, the USA, and other countries. The conference was attended by over 120 participants from 25 countries, including 40 foreign delegates. The Russian participants represented 48 leading research institutions, the foreign delegates work at 30 research institutions and universities all over the world.

 

InterBioScreen, a sponsor and organizer of the Conference, has lent financial support to the younger researchers and post-graduate students.

 

Financial support also came from the International Charitable Foundation Scientific Partnership and other Russian and foreign sponsors:

 

 

The Opening Ceremony started with the salutary address by a full member of the Russian Academy of Natural Sciences, Prof. Prof. V.G. Kartsev, Chairman of Organizing committee.

 

 

At the Conference, the official awarding ceremony of the Medal "In Memory of Prof. A.N. Kost" for 2010 was held.

 

The Medal "In Memory of Prof. A.N. Kost" was instituted in 2005 on the occasion of his 90th Anniversary by the International Charitable Foundation Scientific Partnership, Lomonosov Moscow State University and Russian Mendeleev Chemical Society. The Medal is awarded for outstanding achievements in the chemistry of heterocyclic compounds as a sign of public recognition of the efforts of individual scientists and research groups.

 

The scientists awarded with the Medal in 2010:

 

Prof. Zubenko A.A.	North Caucasian Zonal Research Veterinary Institute, Novocherkassk
Prof. Kartsev V.G.	InterBioScreen
Prof. Preobrazhenskaya M.N.	Gause Institute of New Antibiotics, Russian Academy of Medical Sciences, Moscow
Prof. Rusinov V.L.	Postovsky Institute of Organic Synthesis, Ural Branch of RAS, Yekaterinburg
Prof. Traven' V.F.	Mendeleev University of Chemical Technology, Moscow
Prof. Shults E.E.	Vorozhtsov Institute of Organic Chemistry, Siberian Branch of the RAS, Novosibirsk

 

 

Medal "Badge of Honor" was awarded to

 

 

Prof. Attanasi Orazio A.

University of Urbino “Carlo Bo”, Institute of Organic Chemistry, Italy

 

 

"Gold Badge of International Scientific Partnership Foundation" was awarded to

 

 

Prof. Abdou Wafaa Mahmoud	Ataturk University, Turkey
Prof. Álvarez Mercedes	Institute for Research in Biomedicine (IRB), University of Barcelona, Spain
Prof. Arseniyadis Simeon	Centre National De La Recherche Scientifique, France
Prof. Balci Metin	Middle East Technical University, Turkey
Prof. Bölcskei Hedvig	Gedeon Richter Plc. Medicinal Chemistry II., Hungary
Prof. Botoshansky Mark	TECHNION – Israel Institute of Technology, Israel
Prof. Chung ManChin	School of Pharmaceutical Sciences – University of São Paulo State, Brazil
Prof. Florio Saverio	University of Bari, Italy
Prof. Ganoub Neven Ahamed	National Research Centre, Egypt
Prof. Gautam Dinesh Chandra	University of Rajasthan, India
Prof. Geronikaki Athina	Aristotle University of Thessaloniki, Greece
Prof. Knölker Hans-Joachim	Department Chemie, Technische Universität Dresden, Germany
Prof. Koutentis Panayitis Andreas	University of Cyprus
Prof. López-Calahorra Francisco	University of Barcelona, Spain
Prof. Mąkosza Mieczyslaw	Institute of Organic Chemistry Polish Academy of Sciences, Poland
Prof. Rádl Stanislav	Zentiva, Czech Republic
Prof. Santos Jean Leandro	School of Pharmaceutical Sciences – University of São Paulo State, Brazil
Prof. Saracoglu Nurullah	Ataturk University, Turkey
Prof. Spagnolo Piero	Dipartimento di Chimica Organica “A. Mangini”, Università di Bologna, Italy
Prof. Spinelli Domenico	Dipartimento di Chimica “G. Ciamician”, University of Bologna, Italy
Prof. Stanovnik Branko	University of Ljubljana, Slovenia
Prof. van der Plas Henk	Department of Organic Chemistry, University of Wageningen, the Netherlands
Prof. Yakout EL Sayed M.	Chemical Industries Division, National Research Centre, Egypt
Prof. Yamamoto Yoshinori	Tohoku University, Japan
Executive Secretary Skorova A.E.	Journal "Chemistry of Heterocyclic Compounds", Latvia
Prof. Berestovitskaya V.M.	Herzen State Pedagogical University of Russia, Saint-Petersburg
Prof. Brovarets V.S.	Institute of Bioorganic Chemistry and Petrochemistry NAS of Ukraine, Kiev
Prof. Charushin V.N.	Postovsky Institute of Organic Synthesis, Ural Branch of RAS, Yekaterinburg
Prof. Chupakhin O.N.	Postovsky Institute of Organic Synthesis, Ural Branch of RAS, Yekaterinburg
Prof. Garazd M.M.	Institute of Bioorganic Chemistry and Petrochemistry NAS of Ukraine, Kiev
Prof. Granik V.G.	Center for Chemistry of Medicinal Compounds, Moscow
Prof. Gulevskaya A.V.	Southern Federal University, Rostov-on-Don
Prof. Krasnov K.A.	Institute of Toxicology, Saint-Petersburg
Prof. Levkovskaya G.G.	Favorskii Irkutsk Institute of Chemistry, Siberian Branch of the RAS
Prof. Mikhailovskii A.G.	Perm State Pharmaceutical Academy
Prof. Mikhal'chuk A.L.	Institute of Bioorganic Chemistry, National Academy of Sciences, Minsk, Belarus
Prof. Petrov A.A.	Saint-Petersburg State University
Prof. Poroikov V.V.	Institute of Biomedical Chemistry, Moscow
Prof. Pozharskii A.F.	Southern Federal University, Rostov-on-Don
Prof. Przheval'skii N.M.	Timiryazev State Agricultural University, Moscow
Prof. Ramsh S.M.	Saint-Petersburg State Institute of Technology (Technical University)
Prof. Serov A.B.	Lobachevskii State University, Nizhnii Novgorod
Prof. Shikhaliev Kh.S.	Voronezh State University
Prof. Shklyaev Yu.V	Institute of Technical Chemistry, Ural Branch, Perm'
Prof. Sirakanyan S.N.	Institute of Fine Organic Chemistry NAS RA, Yerevan
Prof. Sukhotin A.V.	Lobachevskii State University, Nizhnii Novgorod
Prof. Tolstikov G.A.	Vorozhtsov Institute of Organic Chemistry, Siberian Branch of the RAS, Novosibirsk
Prof. Vasilevsky S.F.	Institute of Chemical Kinetics and Combustion, Novosibirsk
Prof. Velikorodov A.V.	Astrakhan' State University
Prof. Zefirov N.S.	Moscow State University

 

Prof. van der Plas H.	Prof. Chupakhin O.N.
Prof. Geronikaki A.	Prof. Zefirov N.S.
Prof. Florio S.	Prof. Pozharskii A.F.
Executive Secretary of Journal "Chemistry of Heterocyclic Compounds" Skorova A.E.	Prof. Vasilevsky S.F.

 

By the decision of the Presidium of Russian Academy of Natural Sciences, the V.I. Vernadsky Silver Medal of Honor was awarded to a member of RANS V.G. Kartsev. The medal is awarded for research achievements and significant contribution to the development of Russia.

 

Full member of Russian Academy of Natural Sciences, Prof. Kartsev V.G. (the medal is presented by Member of Presidium of RANS Prof. Pototsky V.V.)

 

 

The Scientific Program started with keynote lectures by the leading experts in the organic chemistry and chemistry of natural compounds:

Van der Plas H.C. (the Netherlands)

Selected reactions in the cyclisation of heterocycles. Cycloalkenopyridines by ring transformation of diazines and triazines

Spinelli D. (Italy)

On the mononuclear rearrangement of heterocycles

Stanovnik B. (Slovenia)
From b-dimethylamino-a-acylamino-a,b-didehydro acid derivatives and related enaminones via heterocycles and heterocyclic amino acids to indole alkaloids

 

The lecture is presented by van der Plas Х.C. (University of Wageningen, the Netherlands)	The lecture is presented by Prof. Spinelli D. (University of Bologna, Italy)
The lecture is presented by Prof. Stanovnik B. (University of Ljubljana, Slovenia)

 

In the reports, and poster sessions were presented original works of Russian and foreign scholars on critical questions of chemistry of heterocyclic compounds, as well as on potentialities for their practical application to solving actual problems of creation of new materials and pharmacologically valuable agents.

The scope and high level of the Conference have been due to excellent plenary lectures delivered by the leading experts in the field.

 

 

The lectures of the plenary session were delivered by:

 

Bruno P., Just-Baringo X., Albericio F., Álvarez M. (Spain)

Total synthesis of natural products with heterocyclic structure

Attanasi O.A. (Italy)

Cultivating over thirty years the passion to build heterocycles from 1,2-diaza-1,3-dienes: the force of imagination

Affortunato F., Degennaro L., Florio S., Giovine A., Luisi R., Mansueto R., Musio B. (Italy)

New horizons in the chemistry of aziridines

Martin R., Agarwal S., Jäger A., Böhl M., Richter S., Tsiavaliaris G., Fedorov R., Manstein D.J., Gutzeit H.O., Knölker H.-J. (Germany)

Specific inhibitors of myosin ATPase via silver-catalyzed synthesis of pyrroles

Mąkosza M., Loska R. (Poland)

Synthesis of perfluoroalkyl heterocycles via nucleophilic substitution of hydrogen

Spagnolo P. (Italy)

Latest applications of aminyl and iminyl radicals derived from azides to the synthesis of nitrogen heterocycles

Yamamoto Y. (Japan)

Coinage metal catalyzed heterocycle synthesis

Charushin V.N., Rusinov V.L., Ovchinnikova I.G., Fedorova O.V.,
Verbitsky E.V., Slepukhin P.A., Chupakhin O.N. (Russia)

Use of tandem and cascade reactions for the synthesis of heterocyclic compounds

Chupakhin О.N., Charushin V.N. (Russia)

S_N^H reactions in heterocyclic chemistry

Poroikov V.V., Filimonov D.A., Lagunin A.A., Gloriozova T.A. (Russia)

Computer-aided prediction of biological activity for natural compounds and their derivatives

Pozharskii A.F., Povalyakhina M.A., Vlasenko M.P. (Russia)

Proton sponge-based heterocyclizations

Preobrazhenskaya М.N. (Russia)

Chemical modification of macrolide antibiotics of oligomycin and amphothericin groups

Shklyaev Yu.V., Rozhkova Yu.S., Vshivkova T.C., Stryapunina O.G., Khmelevskaya K.A. (Russia)

Synthesis of partly hydrogenated nitrogen-containing heterocycles

Vasilevsky S.F., Baranov D.S. (Russia)

New multichannel reactions of acetylenes: an unexpected rearrangement with insertion of nitrogen atom between two acetylenic carbons

Zefirov N.S., Matveeva E.V. (Russia)

Computer and synthetic approaches to novel heterocyclic compounds

 

Oral presentations were made by 24 scientists from Russia and different countries all over the world:

 

Abdou W.M., Khidre M.D., Sediek A.A. (Egypt)

The design and synthesis of sulfur and nitrogen containing bisphosphonic acids and their role in oncology

Arseniyadis S. (France)

From complex oxygen heterocycles to stereodefined carbocycles and chemoselectivity: the domino and chiral pool approaches for biologically active natural product synthesis

Balci M. (Turkey)

Development of new synthetic methodologies for indole, benzoazepinone, furopyrimidinone and furopyrrolone skeleton

Bölcskei H., Gere A., Domány Gy. (Hungary)

Synthesis of diphenyl-triazole and diphenyl-triazine derivatives with COX-2 inhibitory effect

Ganoub N. (Egypt)

Application of phosphorus carbanions in heterocyclic synthesis. An approach to pharmacologically important N- and O-heterocycles and the relevant phosphonate derivatives

Gautam N., Sharma M.K., Gupta S., Ajmera N., Gautam D.C. (India)

Synthesis and biological evaluation of 10H-phenothiazine, 4H-1,4-benzothiazines and their ribofuranosides

Bennamane N., Nedjar-Kolli B., Geronikaki A., Eleftheriou P., Kaoua R., Boubekeur K., Hoffman P., Chaudhaery S.S., Saxena A.K. (Greece)

N-substituted [phenyl-pyrazolo]-oxazin-2-thiones as COX-LOX inhibitors: influence of the replacement of the oxo-group with thioxo-group on the COX inhibition activity of N-substituted pyrazolo-oxazin-2-ones

Koutentis P.A., Gollner A., Lo Re D., Loizou G. (Cyprus)

New routes to azafluoranthenes

Latorre S., Moreira I. de P.R., Bofill J.M., López Calahorra F. (Spain)

Benzothiazole-acridine amines, a new family of multifunctional molecules: from the molecular level to the organic material

Nawwar G. (Egypt)

Simple synthesis of biologically active heterocycles utilizing
3-oxoalkanocarboxylates

Rádl S., Stach J. (Czech Republic)

Synthesis of impurities and/or degradation products of selected heterocyclic drugs as an integral part of the API development

Erdogan E., Kilic H., Bayindir S., Saracoglu N. (Turkey)

Synthesis of possible biological active aza-substituted indoles

Petrov M.L., Androsov D.A. (Russia)

New approaches towards benzofurans, indoles and benzothiophenes

Belovodskii A.V., Shults E.E., Тоlstikov G.А. (Russia)

Palladium-catalyzed arylation of eudesmane type methylene-lactones and their biological activity

Brovarets V.S., Pilyo S.G., Golovchenko A.V., Shablykin O.V., Kozachenko A.P., Prokopenko V.M.,
  Drach B.S.  (Ukraine)

New transformations of 4,5-bifunctionally substituted derivatives of 1,3-oxazole

Demchenko А.М., Kolesnikov А.V., Lozynskii М.О. (Ukraine)

Condensed polymethyleneazoles

Gulevskaya A.V., Tyaglivy A.S., Nguen T.L. Huong (Russia)

Nucleophile-induced cyclizations of mono- and dialkynylpyrazines and pyridazines

Krasnov K.A., Kartsev V.G., Khrustalev V.N. (Russia)

Stereodirected T-reactions of barbituric acid derivatives

Mikhailovskii A.G., Surikova O.V., Polygalova N.N., Aliev Z.G., Vakhrin M.I. (Russia)

Cyclic azomethines and enamines оf 3,4-dihydroisoquinolinium series in heterocyclic synthesis

Gulyakevich O.V., Mikhal'chuk A.L. (Belarus)

Transformations of the 2,3,4,6,7,11b,12,13-octahydro-
1Н-isoquino[2,1-a]quinolin-1,13-diones and related azangular heterocycles in search and creation of new pharmacological agents

Shikhaliev Kh.S., Stolpovskaya N.V., Krylskiy D.V., Liberman M.M., Levina A.M. (Russia)

Heterocyclic systems based on substituted biguanides

Laipanov R.K., Tokmakov G.P., Przheval'skii N.M. (Russia)

Grandberg synthesis of triptamines and its utilization in multicomponent reactions

Shults E.E., Bauman V.T., Тоlstikov G.А. (Russia)

Transition metal catalyzed reactions in the directed synthesis of pharmacological valuable derivatives of morphinane alkaloids

Traven' V.F., Kondratova N.A., Solov'eva N.P. (Russia)

Unusual reactions of 2,3-dihydrofuro[3.2-c]coumarin-3-one, its arylidene and cinnamylidene derivatives with arylhydrazines

 

 

The poster session presented over 40 contributions.

 

 

A high quality edition of the Conference proceedings "Modern Aspects of Chemistry of Heterocycles" (in Russian) continues the series of books "Chemistry and Biological Activity of Synthetic and Natural Compounds". The present volume is a collection of the plenary and oral lectures, as well as the abstracts of poster presentations which review recent achievements in the field of heterocyclic compounds.

 

Editorial Board of the Proceedings

 

Editor-in-chief  Kartsev V.G.

 

International Editorial Board

 

Editorial Board

 

Regional Editors

 

 

 

 

To the attention of the Conference attendants were offered books, published by the general sponsor InterBioScreen at International Charitable Foundation Scientific Partnership’ request: two-volume Proceedings of three Conferences in the heterocycles series: "Nitrogen-Containing Heterocyles and Alkaloids" (СВС2001), "Oxygen- and Sulfur-Containing Heterocycles" (СВС2003), "Nitrogen-Containing Heterocycles" (СВС2006), as well as seven volumes of the periodic series of the monograph "Selected Methods for Synthesis and Modification of Heterocycles" (vol. 1 contains the materials on the chemistry of nitrogen-containing heterocycles, vol. 2 contains the materials on the chemistry of oxygen- and sulfur-containing heterocyles, vol. 3 is devoted to the chemistry of synthetic indole systems, vol. 4 contains the materials on chemistry and biological activity of natural indole systems, vol. 5 is devoted to the chemistry and biological activity of carbolines, vol. 6 presents the data on the chemistry and biological activity of synthetic and natural quinolines, vol. 7 is concerned with methods for synthesis, conversions and biological activity of synthetic isoquinoline systems).

 

Besides, two other books on different subjects were presented: Semenov A.A., Kartsev V.G. "The Fundamentals of Chemistry of Natural Compounds" (for the first time in the Russian literature the book presents the systematic description of chemistry of secondary metabolites – low-molecular substances produced by various species of fauna and flora, their biogenesis, properties and some aspects of their total synthesis) , and Isak A.D., Kartsev V.G. "Chemistry of Naphthostyryls" (the book is devoted to the chemistry of naphthostyryls (naphtholactams) and their derivatives which are used as intermediates in the synthesis of various classes of organic dyes and biologically active compounds).

 

The next, 5^th International conference will be dedicated to centenary anniversary
of Professor N.A. Kost. It is planned for 2015 and will be held in one of
the "Golden Ring" cities.
The conference will focus on the prospects for the development
of chemistry of heterocyclic compounds.