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rok 2006 - Fakulta chemickej a potravinárskej technológie ...

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and stereoselective transformations of bicyclic tetramic acid derivatives. Utilization of such asymmetric<br />

transformation in the synthesis of natural polysubstituted amino acids and their derivatives. Preparation of 5<br />

aryl¬substituted 3 amino-2-hydroxytetrahydrofurans and study of their conversion to optically pure substituted C-<br />

aryl amino¬furanosides.<br />

Project duration: from 01.01.2005 to 31.12.2007<br />

VEGA project No 1/248/05 Polyazaheterocycles and their oxygen analogues. Ecologically<br />

more suitable syntheses, supramolecular structure, biological – physical properties (Viktor<br />

Milata)<br />

The project aims at preparation of novel aromatic polyazaheterocycles on the bases of triazines, dihydropyridines,<br />

pyrimidines, quinolines and quinazolines, having additional fused aromatic or saturated ring. In the early stages of<br />

the project we shall concentrate on preparation of precursors to the above heterocycles by modern, more<br />

ecological methods. Next the precursors will be used in cyclization and cyclocondensation reaction leading to<br />

target compounds. Prepared heterocycles will be modified to enhance their hydrophilicity and hence bioactivity by<br />

attaching a sugar or other hydrophilic moiety. Our attention will concentrate on physicochemical and spectral<br />

characteristics, combined with xray analysis, supramolecular chemistry and quantum chemical calculations.<br />

Project duration: from 01.01.2005 to 31.12.2007<br />

APVV Project No. 20-007304 Synthesis and properties of the pharmacologically potentially<br />

active nitrogen heterocycles (Viktor Milata)<br />

Study and optimisation of the new synthetic methods for preparation of analogues of natural condensed aromatic<br />

polyazaheterocyclic compounds with fused aromatic or saturated ring containing O, S, Se or N atoms.<br />

Preparation of precursors of cited heterocycles and their nitro- and aminoderivatives, imidoylchlorides, imidoyl<br />

and amidinoylisothiocyanates. Exploitation of new precursors in cyclisation and cyclocondesation reactions for<br />

preparation of target compounds. Derivatisation of newly prepared heterocyclic compounds by introduction of<br />

carbohydrate or other hydrophylic part aiming to higher solubility of prepared compounds allowing their more<br />

effective biological application. Study of physico-chemical properties and spectral characteristics of final<br />

derivatives in relation to their X-ray structural analysis, supramolecular chemistry using quantum-chemical<br />

calculations.<br />

Project duration: from 01.01.2005 to 31.12.2007<br />

APVT Project No. 20-000904 Asymmetric Pd(II)-catalysed reactions as a methodology for the<br />

preparation of chiral bulding blocks for the synthesis of biologically active natural<br />

compounds (Peter Szolcsányi)<br />

The main aim of the project is to develop a new and efficient methodology of asymmetric palladium-catalysed<br />

intramolecular and intermolecular aminocarbonylations and halocyclisations for the enantioselective preparation<br />

of optically pure building blocks. These valuable intermediates will serve as suitable chiral precursors for targeted<br />

total syntheses of biologically active natural compounds and/or their analogues with their potential use in human<br />

medicine. The sub-objectives of the project involve the development of a simple and rapid preparation of<br />

necessary aminoalkenitols as starting substrates in multi-gram quantities and required purity, as well as an<br />

effective synthesis of enantiomerically pure chiral Pd-catalysts essential for key asymmetric transformations.<br />

Project duration: from 01.01.2005 to 31.12.2007<br />

VI. COOPERATION<br />

A. Cooperation in Slovakia<br />

Institution Type of cooperation Responsible person Duration<br />

Synkola, Bratislava<br />

Duslo, Šaľa<br />

Slovak Academy of<br />

Sciences, Bratislava<br />

Seminars and conferences<br />

The synthesis of heterocyclic<br />

compounds.<br />

The synthesis of heterocyclic<br />

compounds.<br />

Karvaš Milan, director, Mlynská dolina,<br />

842 15 Bratislava 4<br />

Lehocký Peter, director, Duslo, a. s.<br />

927 03 Šaľa<br />

Tvaroška Igor, director, Dubravská cesta<br />

9, 841 04 Bratislava 4<br />

01.01.1992-<br />

01.01.1990-<br />

01.01.1970<br />

179

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