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Members
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Main topics
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The expertise of the research team is situated in the area of transition metal catalyzed reactions and heterocyclic chemistry (pyridazines, indoles, quinolines, purines). Besides the study of fundamental aspects of transition metal catalyzed reactions (mainly palladium) such as halide effects, base effects, and the influence of molecular heating via microwave irradiation, transition metal catalyzed methods are developed which allow synthesizing (novel) azaheteroaromatic basic skeletons. The new skeletons are interesting "scaffolds" which after specific decoration allow the development of novel enzyme inhibitor and receptor agonist/antagonist. For this purpose we collaborate with academic teams (specialized in medicinal chemistry) and companies. Special attention in the transition metal catalysis work is devoted to the C(sp2)-H bond activation as no carbon-metal (B, Sn, Zn, Mg, ...) or carbon-(pseudo)halogen bond is required for the functionalizations. In addition our group works in the area of nucleophilic substitution of hydrogen where C(sp2)-H bond activation is achieved by the addition of an oxidant in stead of a transition metal catalyst. To support the reaction mechanisms in the homogeneous catalysis work DFT calculations are performed using the supercomputer of the university. This research is performed in collaboration with Prof. Herrebout and Prof. Van der Veken of the University of Antwerp.
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Website
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http://www.ua.ac.be/main.aspx?c=*SCHEIKUN&n=12202&ct=007999&e=t16642
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Projects
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Show the projects of this research team - Direct alkylation of saturated cyclic amines via catalytic C-H functionalization (DASCA). 01/03/2013 - 28/02/2015
| Abstract | The project aims to develop truly practical and scalable synthetic methods with a broad functional group compatibility for the direct catalytic α-functionalization of C(sp3)-H species next to nitrogen. Such methodology will have a tremendous ompact on the way synthetic chemists approach the construction and derivatization of complex molecules comprising saturated cyclic amines. Additionally, the wide diversity of such a type heterocycles provides a broad scope of substrates for combinatorial synthesis. | | Duration | 01/03/2013 - 28/02/2015 | | Researcher(s) | | | Research Team(s) | |
- Peptide diversification: Pd-catalyzed derivatization of lead compounds in aqueous medium. 01/01/2013 - 31/12/2017
| Abstract | This project represents a research agreement between the UA and on the onther hand IWT. UA provides IWT research results mentioned in the title of the project under the conditions as stipulated in this contract. | | Duration | 01/01/2013 - 31/12/2017 | | Researcher(s) | | | Research Team(s) | |
- Development of new sustainable Cu- and Fe-catalyzed oxidation reactions. 01/01/2013 - 31/12/2016
| Abstract | In the framework of this research project new aerobic Cu- and Fe-catalyzed oxidation reactions will be developed which allow transformation of aryl(heteroaryl)- and bis(heteroaryl)methanes/alkanes into the corresponding ketones and alcohols. The oxidation
methods aim at a high atom efficiency, a low E-factor and are based on cheap base metals. | | Duration | 01/01/2013 - 31/12/2016 | | Researcher(s) | | | Research Team(s) | |
- Chemical Manufacturing Methods for the 21st Century Pharmaceuticals Industries (CHEM21). 01/11/2012 - 31/10/2016
| Abstract | CHEM21 is a project that will develop a broad based portfolio of sustainable technologies for green chemical intermediate manufacture aimed at the pharmaceutical industry. Initially working with the EFPIA members the collaborators of CHEM21 will analyse a number of projects that are in development to decide which the priorities are for technology development. | | Duration | 01/11/2012 - 31/10/2016 | | Researcher(s) | | | Research Team(s) | |
- Development of new synthetic methods for the preparation of amidines and guanidines. 01/10/2012 - 30/09/2013
| Abstract | In the framework of this project, we want to develop new synthetic methods for (hetero)arenecarboximidamides and guanidines. More specifically transition metal catalyzed strategies involving the use of isonitriles, (hetero)arenes/chloro(hetero)arylzincs and
amines/chloroamines for the (hetero)arenecarboximidamide construction, and isonitriles and amines/chloroamines for the guanidine build up will be explored. | | Duration | 01/10/2012 - 30/09/2013 | | Researcher(s) | | | Research Team(s) | |
- Separation, recovery and re-use of organotin derivatives. 05/01/2012 - 04/01/2013
| Abstract | Organotin derivatives form a very important class of reagents in the organic synthetic chemistry. Due to the toxicity of the currently used organotin reagents, the difficult purification of the reaction products and the problem to recover and re-use the formed tin waste in a simple manner the industrial applications are hitherto limited. This project describes a simple though sustainable solution for the triple problem. | | Duration | 05/01/2012 - 04/01/2013 | | Researcher(s) | | | Research Team(s) | |
- Transition metal catalyzed transformation of amides. 01/01/2012 - 31/12/2015
| Abstract | In the framework of this project synthetic methodology for the transformation of secondary amides into secondary amines will be developed. The new methodology is based on the use of transition metal catalysis and a sustainable hydride donor.
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- FunMem4Affinity: Exploration of functional ceramic membranes for affinity organic solvent nanofiltration. 01/01/2012 - 31/12/2014
| Abstract | The main objective of the project FunMem4Affinity is the exploration and understanding of the potential of affinity separation with functionalized ceramic membranes in nanofiltration in organic solvents. | | Duration | 01/01/2012 - 31/12/2014 | | Researcher(s) | | | Research Team(s) | |
- Development of new benzo[g]isochinoline-5,10-dion derivatives as potential antiplasmodial and antimycobacterial compounds. 01/01/2012 - 31/12/2013
| Abstract | This project represents a research agreement between the UA and on the onther hand IWT. UA provides IWT research results mentioned in the title of the project under the conditions as stipulated in this contract. | | Duration | 01/01/2012 - 31/12/2013 | | Researcher(s) | | | Research Team(s) | |
- New azole fused purines: synthesis, derivatization and biological evaluation. 01/01/2012 - 31/12/2013
| Abstract | This project represents a research agreement between the UA and on the onther hand IWT. UA provides IWT research results mentioned in the title of the project under the conditions as stipulated in this contract. | | Duration | 01/01/2012 - 31/12/2013 | | Researcher(s) | | | Research Team(s) | |
- Direct C-H bond functionalization reactions: development of procedures to remove a pyridine directing group 01/01/2012 - 31/12/2012
| Abstract | Direct C(sp³)-H functionalizations alfa to nitrogen in aliphatic amines can be efficiently achieved when pyridine is involved as a directing group (DG). Pyridine is however a stable directing group and was therefore considered to be irremovable after the functionalization step. This project focuses on the development on pyridine removal strategies. | | Duration | 01/01/2012 - 31/12/2012 | | Researcher(s) | | | Research Team(s) | |
- Azaheteroaromatic Scaffold Design via Transition Metal-Catalyzed C-H Bond Activation and Their Application in Medicinal Chemistry (FWO Vis. Fel., Pradip DEBNATH, India). 01/12/2011 - 30/11/2012
| Abstract | This is a fundamental research project financed by the Research Foundation - Flanders (FWO). The project was subsidized after selection by the FWO-expert panel. | | Duration | 01/12/2011 - 30/11/2012 | | Researcher(s) | | | Research Team(s) | |
- Visiting Postdoctoral Fellowship (Santanu CHAKRAVORTY, India) 01/12/2011 - 30/11/2012
| Abstract | Visiting Postdoctoral Fellowship under the project "Selection of bioactive quinoids and analysis of a combined drug therapy and immunoprophylaxis for the control of turberculosis". | | Duration | 01/12/2011 - 30/11/2012 | | Researcher(s) | | | Research Team(s) | |
- Transition metal catalyzed transformation of amides. 01/10/2011 - 30/09/2014
| Abstract | In this project new synthetic methodology will be developed for the transition metal catalyzed transformation of amides into other functional groups; amines. In the research attention will be given to the unravelling of the reaction mechanism of the new synthetic processes. | | Duration | 01/10/2011 - 30/09/2014 | | Researcher(s) | | | Research Team(s) | |
- Development of a new domino aza-Cope rearrangement − reductive coupling of N-homoallyl aldimines and alkynes: a DOS approach for the synthesis of new functionalised (homo)allylamines. 01/10/2011 - 30/09/2012
| Abstract | We will develop new domino reactions for the synthesis of a structurally diverse collection of allylic, propargylic and homoallylic amines and aza-heterocyclic compounds. A cationic 2-aza-Cope rearrangement of α,α-dihalogenated N-homoallylaldimines, followed by a Lewis acid catalyzed reductive coupling with an alkyne leads to the title products. The use of α,α,ω-trihalogenated N-homoallylaldimines will lead to aza-heterocycles. | | Duration | 01/10/2011 - 30/09/2012 | | Researcher(s) | | | Research Team(s) | |
- FWO Visiting Postdoctoral Fellowship (Satyajit SAHA, Netherlands) 15/02/2011 - 14/02/2012
| Abstract | The key goal of this project is to synthesise as expeditiously as possible a wide variety of functionalized aza-anthraquinones and to test them. | | Duration | 15/02/2011 - 14/02/2012 | | Researcher(s) | | | Research Team(s) | |
- BOF: 1 year doctoral fellowship. 01/01/2011 - 31/12/2011
| Abstract | This project represents a research contract awarded by the University of Antwerp. The supervisor provides the Antwerp University research mentioned in the title of the project under the conditions stipulated by the university. | | Duration | 01/01/2011 - 31/12/2011 | | Researcher(s) | | | Research Team(s) | |
- Synthesis of benzodiazines based on C-N bond formation via transition metal-catalyzed C(sp2)-H activation. 01/10/2010 - 30/09/2014
| Abstract | The project aims the development of new synthetic methods for the synthesis of benzodiazines. The intention is to form the C-N bond using transition metal catalyzed C-H activation. By using C-H activation there is no need for pre-activation, which shortens the number of reaction steps and creates less waste. | | Duration | 01/10/2010 - 30/09/2014 | | Researcher(s) | | | Research Team(s) | |
- Synthesis and biological evaluation of novel pyridazin-3(2H)-one derivatives. 28/08/2010 - 27/06/2011
| Abstract | Halogen-metal exchange and direct metalation followed by reactions with electrophiles, in order to functionalize the biologically relevant pyridazin-3(2H)-one core will be studied. | | Duration | 28/08/2010 - 27/06/2011 | | Researcher(s) | | | Research Team(s) | |
- Testing and evaluation of compounds for properties useful for agricultural and horticultural crop protection agents or useful for applications in animal health and professional products. 28/05/2010 - 27/05/2013
| Abstract | This project represents a formal service agreement between UA and on the other hand Du Pont de Nemours. UA provides Du Pont de Nemours research results on "Testing and evaluation for agricultural and horticultural crop protection ¿" under the conditions as stipulated in the document. | | Duration | 28/05/2010 - 27/05/2013 | | Researcher(s) | | | Research Team(s) | |
- Selection of bioactive quinoids and analysis of a combined drug therapie and immunoprophylaxis for the control of tuberculosis. 01/02/2010 - 31/12/2013
| Abstract | This research proposal aims to (1) design innovative syntheses of new bioactive 2-azaanthraquinones (UGent, VUB), (2) evaluate specific functionalization of the 2-azaanthraquinone skeleton with respect to a SAR-study until compounds are obtained with a desired profile of bioactivity (UGent, VUB), (3) test the in vitro and in vivo toxicity of these components and their pharmacokinetics (WIV), (4) test their in vivo bacteriostatic and bactericidal potential against M. tuberculosis (WIV), (5) test their therapeutic potential in two in vivo models of latent tuberculosis in combination with post-exposure vaccination with plasmid DNA (WIV). | | Duration | 01/02/2010 - 31/12/2013 | | Researcher(s) | | | Research Team(s) | |
- Research in heterocyclic chemistry. 01/02/2010 - 31/12/2011
| Abstract | This project represents a research contract awarded by the University of Antwerp. The supervisor provides the Antwerp University research mentioned in the title of the project under the conditions stipulated by the university. | | Duration | 01/02/2010 - 31/12/2011 | | Researcher(s) | | | Research Team(s) | |
- Azaheteroaromatic Scaffold Design via Transition Metal-Catalyzed C-H Bond Activation and Their Application in Medicinal Chemistry. 01/01/2010 - 31/12/2013
| Abstract | This is a fundamental research project financed by the Research Foundation - Flanders (FWO). The project was subsidized after selection by the FWO-expert panel. | | Duration | 01/01/2010 - 31/12/2013 | | Researcher(s) | | | Research Team(s) | |
- Integrated organic-inorganic synthetic approaches for the development of functionalized periodic mesoporous organosilicas. 01/01/2010 - 31/12/2013
| Abstract | Innovative synthetic approaches for the formation of strongly functionalized crystalline ''Periodic Mesoporous Organosilicas'' (PMO''s) will be developed. Knowledge and reactions from organic chemistry will be implemented in the known synthesis processes for the production of porous hybrid organic-inorganic materials.
Therefore, 2 synthesis paths will be established. 1) On one hand, new organosilica precursors with embedded heteroatoms (N, S, O, P, Cl, ¿) will be synthesized, that can be applied in the synthesis of the innovative PMO''s. 2) Another synthesis path aims at executing organic reactions, known in homogeneous reaction media, inside the formed crystalline aromatic-bridged PMO in order to modify the aromatic functions of the PMO. Emphasis will be put on the fundamental aspects such as the influence of the present heteroatoms on the synthesis mechanism of the PMO''s. | | Duration | 01/01/2010 - 31/12/2013 | | Researcher(s) | | | Research Team(s) | |
- Synthesis of bicyclic azaheteroaromatics based on C-N bond formation via transition metal-catalyzed C(sp2)-H activation. 01/01/2010 - 31/12/2010
| Abstract | The project aims the development of new synthetic methods for the synthesis of azaheteroaromatics. The intention is to form the C-N bond using transition metal catalyzed C-H activation. By using C-H activation there is no need for pre-activation, which shortens the number of reaction steps and creates less waste. | | Duration | 01/01/2010 - 31/12/2010 | | Researcher(s) | | | Research Team(s) | |
- Synthesis and biological evaluation of (+)-epiquinamide and analogues. 01/10/2009 - 30/09/2013
| Abstract | This project represents a research contract awarded by the University of Antwerp. The supervisor provides the Antwerp University research mentioned in the title of the project under the conditions stipulated by the university. | | Duration | 01/10/2009 - 30/09/2013 | | Researcher(s) | | | Research Team(s) | |
- Microwave-assisted chemical valorisation of biomass and bio-raw materials. 01/09/2009 - 31/08/2011
| Abstract | First, the microwave-assisted synthesis (with or without heterogeneous catalyst) of renewable chemicals starting from plant oil and animal fat (triglycerides) or derivatives of triglycerides (free fatty acids) will be studied. Secondly, the design and
the construction of a continuous microwave reactor will take place. | | Duration | 01/09/2009 - 31/08/2011 | | Researcher(s) | | | Research Team(s) | |
- Development of methods for the efficient synthesis of functionalisation of heterocyclic "scaffolds". 01/08/2009 - 31/07/2014
| Abstract | The research plan is situated in the area of organometallic and heterocyclic chemistry. Besides the study of fundamental aspects of transition metal catalyzed reactions, transition metal catalyzed methods will be developed which will allow the synthesis of (novel) heteroaromatic skeletons. These skeletons are interesting scaffolds which after specific decoration are useful in the development process of new drugs and agrochemicals. Special attention in the transition metal catalysis work will be devoted to the C-H (sp2 and sp3) bond activation. In addition C(sp2)-H bond activation via nucleophilic substitution of hydrogen, by the addition of an oxidant instead of a transition metal catalyst, will also be covered. As an extension of the previous research devoted towards the C-functionalization of the pyridazinone core via Pd-catalyzed cross-coupling reactions, the potential of metal-halogen exchange with RMgX will be explored. | | Duration | 01/08/2009 - 31/07/2014 | | Researcher(s) | | | Research Team(s) | |
- * Organica. 01/04/2009 - 31/03/2013
| Abstract | This project represents a research contract awarded by the University of Antwerp. The supervisor provides the Antwerp University research mentioned in the title of the project under the conditions stipulated by the university. | | Duration | 01/04/2009 - 31/03/2013 | | Researcher(s) | | | Research Team(s) | |
- Microwave assisted synthesis of renewable raw materials from triglycerides. 01/01/2009 - 31/12/2010
| Abstract | Study of the microwave assisted synthesis of renewable raw materials from triglycerides with specific attention for new catalysts and catalyst-free processes. These processes reduce the amount of waste products and they could also be the start of the development of compact industrial production processes (flow-through microwave reactors). | | Duration | 01/01/2009 - 31/12/2010 | | Researcher(s) | | | Research Team(s) | |
- Synthesis, decoration and biological evaluation of new anellated purines. 01/01/2009 - 31/12/2010
| Abstract | No abstract found | | Duration | 01/01/2009 - 31/12/2010 | | Researcher(s) | | | Research Team(s) | |
- Topics in heterocyclic chemistry. 01/12/2008 - 30/11/2013
| Abstract | This project represents a formal research agreement between UA and on the other hand a private institution. UA provides the private institution research results mentioned in the title of the project under the conditions as stipulated in this contract. | | Duration | 01/12/2008 - 30/11/2013 | | Researcher(s) | | | Research Team(s) | |
- Development of Pd-catalyzed cross-coupling reactions and the effect of additives on the reaction rate. 01/10/2008 - 20/09/2009
| Abstract | No abstract found | | Duration | 01/10/2008 - 20/09/2009 | | Researcher(s) | | | Research Team(s) | |
- Stille reactions: Study of a new halide effect and development of a new approach for the efficient removal of trialkyltin halides. 01/01/2008 - 31/12/2010
| Abstract | In this project the effect of halide ions on the rate and mechanism of Stille reactions will be investigated. In addition an alternative aproach for the separation of trialkyltinhalogenide from the reaction product will be optimized. | | Duration | 01/01/2008 - 31/12/2010 | | Researcher(s) | | | Research Team(s) | |
- Synthesis and evaluation of derivatives of 5-methyl-5H-indolo [2,3-c] quinoline (isoneocryptolepine); a new antiplasmodial indoloquinoline. 01/01/2008 - 31/12/2009
| Abstract | The aim of this project is three-fold. First we will optimize the synthesis of the isoneocryptolepine skeleton. For this purpose, we will use a recently (by our lab) developed procedure: a consecutive or tandem Buchwald-Hartwig amination - intramolecular Pd-catalyzed arylation. We will also apply this method for our second goal: the synthesis of D-ring substituted isoneocryptolepines. We prefer the aminoalkylamino- or aminoalkylgroup, because of their indispensable importance for the drug chloroquine. Finally, we will also synthesize ring-modified isoneocryptolepines: removal of the D-ring, reduction of the D-ring and the synthesis of the isoquinoline isomer of isoneocryptolepine. On this last mentioned isomer, we will also remove and reduce the D-ring. | | Duration | 01/01/2008 - 31/12/2009 | | Researcher(s) | | | Research Team(s) | |
- Synthesis of novel pyridazinone compounds. 06/12/2007 - 05/12/2012
| Abstract | Project in collaboration with the industry. | | Duration | 06/12/2007 - 05/12/2012 | | Researcher(s) | | | Research Team(s) | |
- Heterocyclic synthesis medicinal and supramolecular chemistry. (FWO Vis. Fel., Oksana RYABTSOVA, Russia) 01/09/2007 - 31/08/2008
| Abstract | No abstract found | | Duration | 01/09/2007 - 31/08/2008 | | Researcher(s) | | | Research Team(s) | |
- Heterocyclic synthesis in medicinal and supramolecular chemistry. 01/01/2007 - 31/12/2011
| Abstract | In the frame of a ''Scientific Research Community ''of the ''Fund for Scientific Research Flanders'' (FWO-Flanders) research laboratories of KuLeuven, UG, VUB and UA will collaborate on the topics:
- New methodologies in heterocyclic chemistry
- Medicinal chemistry based on heterocyclic components
- Supramolecular chemistry based on heterocyclic skeletons | | Duration | 01/01/2007 - 31/12/2011 | | Researcher(s) | | | Research Team(s) | |
- Synthesis, decoration and biological evaluation of new anellated purines. 01/01/2007 - 31/12/2008
| Abstract | No abstract found | | Duration | 01/01/2007 - 31/12/2008 | | Researcher(s) | | | Research Team(s) | |
- Study of a new halide effect in palladium catalyzed C-C bond forming reactions and development of new antiplatelet agents based on a pyridazin-3(2H)-one skelet. 01/10/2006 - 30/09/2008
| Abstract | No abstract found | | Duration | 01/10/2006 - 30/09/2008 | | Researcher(s) | | | Research Team(s) | |
- Study of the Transesterification of Triglycerides with Mono-alcohols under Microwave Heating. 01/01/2006 - 31/12/2007
| Abstract | Study of the transesterification of triglycerides with mono-alcohols under microwave heating, aiming increased conversion and reaction speed, as well as the use of lower (up to zero) concentration of catalyst. Realization of these targets would lead to cheaper biodiesel production, to cheaper fatty acid esters of higher alcohols (higher added value), to a reduction of effluents during downstream processing and to more compact industrial production processes (flow-through reactors). | | Duration | 01/01/2006 - 31/12/2007 | | Researcher(s) | | | Research Team(s) | |
- Synthesis and evaluation of derivatives of 5-methyl-5H-indolo [2,3-c] quinoline (isoneocryptolepine); a new antiplasmodial indoloquinoline. 01/01/2006 - 31/12/2007
| Abstract | The aim of this project is three-fold. First we will optimize the synthesis of the isoneocryptolepine skeleton. For this purpose, we will use a recently (by our lab) developed procedure: a consecutive or tandem Buchwald-Hartwig amination - intramolecular Pd-catalyzed arylation. We will also apply this method for our second goal: the synthesis of D-ring substituted isoneocryptolepines. We prefer the aminoalkylamino- or aminoalkylgroup, because of their indispensable importance for the drug chloroquine. Finally, we will also synthesize ring-modified isoneocryptolepines: removal of the D-ring, reduction of the D-ring and the synthesis of the isoquinoline isomer of isoneocryptolepine. On this last mentioned isomer, we will also remove and reduce the D-ring. | | Duration | 01/01/2006 - 31/12/2007 | | Researcher(s) | | | Research Team(s) | |
- Synthesis of Aminoalkylamino-substituted Neocryptolepine Analogues: Valorisation of the Cryptolepine Alkaloids as Antimalarials. 01/01/2006 - 31/12/2007
| Abstract | The aim of this project is the synthesis of aminoalkylamino substituted neocryptolepine derivatives. Herewith we aim to decrease the cytotoxicity and to increase the antiplasmodial activity of the natural product neocryptolepine. These substituted neocryptolepines will be prepared from the corresponding chloroneocryptolepines using a Buchwald-Hartwig amination. 1-, 2-, 3-, 4-, 7-, 8-, 9-, 10- and 11-chloroneocryptolepine will be synthesized via respectively a ''condensation - Graebe-Ullmann'', a ''Palladium catalyzed amination - arylation'' and a ''Friedel-Crafts acylation - intramolecular nitrene C-H insertion'' approach. | | Duration | 01/01/2006 - 31/12/2007 | | Researcher(s) | | | Research Team(s) | |
- of New Platelet Aggregation Inhibitors based on a Pyridazin-3(2H)-one core. 01/01/2006 - 30/06/2006
| Abstract | The effect of substitution on the C-4 position of 2-methyl-5-[(1E)-3-oxo-3-phenylprop-1-en-1-yl]pyridazin-3(2H)-one on the platelet aggregation inhibition will be investigated. In addition the influence of moving the 3-oxo-3-phenylprop-1-en-1-yl group on C-5 to C-4 and C-6, as well as substitution of this group for a (phenylsulfinyl)vinyl-, a (phenylsulfonyl)vinyl- and a (diphenylphosphoryl)vinyl group will be studied. | | Duration | 01/01/2006 - 30/06/2006 | | Researcher(s) | | | Research Team(s) | |
- Investigation of New Fundamental Aspects of Palladium-Catalyzed Reactions and their Practical Application in Organic Syntheses. 01/05/2005 - 30/04/2009
| Abstract | In this research proposal two new fundamental aspects of palladium-catalyzed reactions are investigated ("base effect" and "transhalogenation") and their practical application in organic syntheses. Moreover, partly based on the knowledge of the "base effect", tandem Pd-catalyzed N arylation- and tandem Pd-catalyzed N and C arylation protocols will be developed to allow the efficient synthesis of (substituted) polycyclic azaheteroaromatic skeletons. | | Duration | 01/05/2005 - 30/04/2009 | | Researcher(s) | | | Research Team(s) | |
- Nucleophilic Substitution of Hydrogen under Temperature-Controlled Microwave Heating. 01/04/2005 - 31/12/2005
| Abstract | In this project alternative reagents for SNH amination reactions such as the Chichibabin reaction and the oxidative amino-dehydrogenation will be investigated. The effect of fast and homogeneous heating by microwave radiation on s-adduct formation and rearomatization will be investigated. The new reaction conditions have to avoid the drawbacks of the cited reactions and combine the advantages. | | Duration | 01/04/2005 - 31/12/2005 | | Researcher(s) | | | Research Team(s) | |
- Synthesis and evaluation of derivatives of 5-methyl-5H-indolo[2,3-c]quinoline (isoneocryptolepine); a new antiplasmodial indoloquinoline. 01/01/2005 - 31/12/2005
| Abstract | In this project we aim the synthesis of aminoalkylamino- and aminoalkyl- substituted isoneocryptolepines as potential new antiplasmodial compounds. A new synthetic method will be developed for the indoloquinoline skeleton based on modern palladium-catalyzed reactions. D-ring modified derivatives of isoneocryptolepine will also be synthesized and evaluated on their antiplasmodial activity. | | Duration | 01/01/2005 - 31/12/2005 | | Researcher(s) | | | Research Team(s) | |
- Pyridazine Derivates : Investigation of new methods for the direct introduction of carbon substituents and study of a new halide effect in palladium catalyzed C-C bond forming reactions. 01/10/2004 - 30/09/2006
| Abstract | In this project a new effect of halide anions on transition metal catalysed reactions will be investigated. In addition, new methods for the C-functionalisation of the pyridazine nucleus will be studied via metal-halogen exchange. | | Duration | 01/10/2004 - 30/09/2006 | | Researcher(s) | | | Research Team(s) | |
- Investigation of the effect of temperature controlled microwave flash heating on the reaction rate of palladium catalyzed reactions with chlorinated azaheteroaromatic substrates. 01/01/2004 - 31/12/2006
| Abstract | No abstract found | | Duration | 01/01/2004 - 31/12/2006 | | Researcher(s) | | | Research Team(s) | |
- Synthesis of Aminoalkylamino-substituted Neocryptolepine Analogues: Valorisation of the Cryptolepine Alkaloids as Antimalarials. 01/01/2004 - 31/12/2005
| Abstract | The aim of this project is the synthesis of aminoalkylamino substituted neocryptolepine derivatives. Herewith we aim to decrease the cytotoxicity and to increase the antiplasmodial activity of the natural product neocryptolepine. These substituted neocryptolepines will be prepared from the corresponding chloroneocryptolepines using a Buchwald-Hartwig amination. 1-, 2-, 3-, 4-, 7-, 8-, 9-, 10- and 11-chloroneocryptolepine will be synthesized via respectively a ''condensation - Graebe-Ullmann'', a ''Palladium catalyzed amination - arylation'' and a ''Friedel-Crafts acylation - intramolecular nitrene C-H insertion'' approach. | | Duration | 01/01/2004 - 31/12/2005 | | Researcher(s) | | | Research Team(s) | |
- Investigation of new methods for the direct introduction of carbon substituents on the pyridazin-3(2H)-one skeleton via organometallic chemistry. 01/10/2003 - 30/09/2004
| Abstract | No abstract found | | Duration | 01/10/2003 - 30/09/2004 | | Researcher(s) | | | Research Team(s) | |
- No title found 01/10/2003 - 31/12/2003
| Abstract | No abstract found | | Duration | 01/10/2003 - 31/12/2003 | | Researcher(s) | | | Research Team(s) | |
- No title found 01/10/2003 - 31/12/2003
| Abstract | No abstract found | | Duration | 01/10/2003 - 31/12/2003 | | Researcher(s) | | | Research Team(s) | |
- No title found 01/10/2003 - 30/09/2005
| Abstract | No abstract found | | Duration | 01/10/2003 - 30/09/2005 | | Researcher(s) | | | Research Team(s) | |
- No title found 01/10/2003 - 30/04/2004
| Abstract | No abstract found | | Duration | 01/10/2003 - 30/04/2004 | | Researcher(s) | | | Research Team(s) | |
- No title found 01/10/2003 - 31/12/2003
| Abstract | No abstract found | | Duration | 01/10/2003 - 31/12/2003 | | Researcher(s) | | | Research Team(s) | |
- Submitting novel chemical compounds in accordance with the research strategy defined by the team. 01/10/2003 - 31/10/2003
| Abstract | No abstract found | | Duration | 01/10/2003 - 31/10/2003 | | Researcher(s) | | | Research Team(s) | |
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