Dissertations / Theses on the topic 'Pyridazinone'
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Greenwood, Jeremy R. (Jeremy Robert) 1971. "Pyridazinediones and amino acid receptors theoretical studies, design, synthesis and evaluation of novel analogues." [Sydney : J. Greenwood], 1999. http://www.pharmacol.usyd.edu.au/thesis.
Full textGreenwood, Jeremy Robert. "Pyridazinediones and amino acid receptors: theoretical studies, design, synthesis, and evaluation of novel analogues." Thesis, The University of Sydney, 1999. http://hdl.handle.net/2123/394.
Full textGreenwood, Jeremy Robert. "Pyridazinediones and amino acid receptors: theoretical studies, design, synthesis, and evaluation of novel analogues." University of Sydney, Department of Pharmacology, 1999. http://hdl.handle.net/2123/394.
Full textMoniot, Aurélie. "Etude des effets anti-inflammatoires et anti-cancéreux de nouvelles molécules agrosourcées à motif pyridazinone Synthesis and biological evaluation of pyridazinone derivatives as potential antiinflammatory agents Osteoinductive Material to Fine-Tune Paracrine Crosstalk of Mesenchymal Stem Cells With Endothelial Cells and Osteoblasts." Thesis, Reims, 2020. http://www.theses.fr/2020REIMS022.
Full textOsteosarcoma is a rare primary bone cancer for which current therapeutic approaches are unfortunately insufficient to provide a total cure. So the need for new molecules development is constant. In addition, after tumor excision, bone defect may require materials to fill and support bone rebuilding. The inflammatory potential of such materials is well documented. Phosphodiesterase type 4 inhibitors, including pyridazinone-scaffold based molecules, have already proven themselves as anti-cancer and anti-inflammatory agents in a number of in vitro models. The goal of this work was to assess the anti-cancer and anti-inflammatory effects of new pyridazinone-scaffold based molecules derived from agrosourced precursors. Anti-inflammatory effects have been assessed on cytokine production, migratory potential and the phagocytic abilities of human primary neutrophils in vitro and in an in vivo model of inflammation in mice. These molecules have also shown their therapeutic potential in in vitro osteosarcoma models where they decreased cell proliferation and migration while inducing apoptosis in cancer cells. In vivo, these molecules were able to decrease tumor growth and maintain mineral bone quality. These results indicated that new pyridazinone scaffold-based molecules might be integrated into a multi-therapy, both for their anti-cancer and anti-inflammatory therapeutic potential
Goedhart, Christian Leonard. "Influence of osmotic stress, ethanol, and a substituted pyridazinone, BAS 13-338, on the growth and lipid composition of two Chlorella species." Diss., Virginia Polytechnic Institute and State University, 1987. http://hdl.handle.net/10919/53634.
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Byrichetti, Kiranmai. "Synthesis and Structure of a Substituted Pyridazine." TopSCHOLAR®, 2011. http://digitalcommons.wku.edu/theses/1080.
Full textGuven, Alaettin. "Potentially tautomeric pyridazino(4, 5-b)indolones." Thesis, University of East Anglia, 1992. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.306148.
Full textGreenwood, Jeremy R. "Pyridazinediones and amino acid receptors theoretical studies, design, synthesis and evaluation of novel analogues /." [Sydney : J. Greenwood], 1999. http://www.pharmacol.usyd.edu.au/thesis.
Full textTitle from title screen. Interactive three dimensional molecular data and multiple colour images. Text presented in Hypertext Markup Language (.htm); images in standard formats (.jpg, .gif); molecules presented mostly as Cambridge Protein Data Bank format (.pdb); some molecules presented in alternative X. Mol cartesian co-ordinates format (.xyz); search facility in PERL script. Includes bibliographical references. A printed form was produced with limited features as a Faculty requirement; may also be issued in CD-ROM.
Mernari, Bouchaïb. "Complexes binucléaires de dérivés de la pyridazyne ou du pyrazole : synthèses, structures cristallines et interactions magnétiques." Lille 1, 1987. http://www.theses.fr/1987LIL10015.
Full textFoster, Joshua B. "Development of Pyridazine-Derivatives for the Treatment of Neurological Disorders." The Ohio State University, 2019. http://rave.ohiolink.edu/etdc/view?acc_num=osu1545904228813231.
Full textTran, Gaël. "Synthèse de phosphonylpyrazoles et de fluoropyridazines." Thesis, Paris 6, 2015. http://www.theses.fr/2015PA066414/document.
Full textThe work presented in this manuscript concerns the development of synthetic routes to two families of heterocycles, namely phosphonylpyrazoles and fluoropyridazines. Phosphonylpyrazoles were synthesized using a Hirao-type cross-coupling, and it was demonstrated during this study that a single catalytic system based on Pd(OAc)2/XantPhos could perform the cross-coupling between a wide range of halopyrazoles and H-phosphonyls. Significant limits have been met in the scope of this method, especially regarding the substitution pattern of the halopyrazole. Nevertheless, at this time, this method is arguably one of the most flexible ways to synthesize phosphonylpyrazoles. Fluoropyridazines were synthesized using a [2+1]/[3+2] cycloaddition sequence between alkynes, the difluorocarbene :CF2, and alkyl diazoacetates. It was demonstrated during this study that a wide range of alkynes could be involved in this sequence, and that the corresponding 5-fluoropyridazines could be easily diversified
Bakkali, Hicham. "Synthèse d'analogues pyrroliques par régression de cycle thiaziniques et pyridaziniques : application pour l'élaboration de nouveaux ligands pyridaziniques et pyrroliques." Nantes, 2005. http://www.theses.fr/2005NANT2132.
Full textVaccarella, Graziano. "Synthesis and activity of pyridazine analogues of the excitatory neurotransmitter, glutamic acid." Thesis, The University of Sydney, 1998. https://hdl.handle.net/2123/27573.
Full textBrandl, Doris. "Mehrstufige Diels-Alder-Reaktionen von Acceptor-substituierten Pyridazinen mit 2-Cyclopropyliden-1,3-dimethylimidazolidin." Diss., [S.l.] : [s.n.], 2002. http://edoc.ub.uni-muenchen.de/archive/00000121.
Full text林浩強 and Ho-keung Lam. "Inhibitory effect of tetramethylpyrazine (TMP) on nitric oxide production in macrophages." Thesis, The University of Hong Kong (Pokfulam, Hong Kong), 2001. http://hub.hku.hk/bib/B31970163.
Full textMojovic, Ljubica. "Métallations et synthèses en série pyrazinique et pyridazinique." Rouen, 1990. http://www.theses.fr/1990ROUES033.
Full textAreschka, Vincent. "Syntèse et oxydation de la 1-amino-4,7-dimethyl-1h-v-triazolo[4,5]pyridazine." Doctoral thesis, Universite Libre de Bruxelles, 1991. http://hdl.handle.net/2013/ULB-DIPOT:oai:dipot.ulb.ac.be:2013/213049.
Full textUrgin, Karene. "Préparation de dérivés aryl- et hétéroaryl- pyridazine(s) par voies organométalliques chimiques ou électrochimiques." Thesis, Paris Est, 2010. http://www.theses.fr/2010PEST1094.
Full textHeteroaromatic rings are present in various biological and pharmacological active molecules. Substituted aryl-pyridazines have given rise to considerable interest because of their diverse pharmacological properties (antibacterial, anti-inflammatory, cardiovascular drugs…). Moreover, structures which contain pyridazines are used in supramolecular chemistry for their applications through self-assembly processes in the presence of metal ions.In order to elaborate building blocks containing pyridazine rings such as aryl or heteroaryl-pyridazines, we turned our intention on the development of complementary methods involving organometallic reagents. Transition metal-catalyzed cross-coupling reaction of organometallic compounds with organic halides is one of the most powerful methods for the generation of C-C bonds.We chose to develop the most straightforward method involves heterocoupling reaction of aryl/heteroaryl compounds under electrochemical conditions (sacrificial anode process) associated to a nickel catalysis. However some limitations have been pointed out when 3,6-dihalogenopyridazines are involved in the cross-coupling reaction. An electrochemical study was investigated in order to propose some mechanistic considerations. A second part of this work consisted in the study of arylzinc and triarylbismuths reagents toward 3,6-dihalogenopyridazines
Mackrell, Alexander David. "Towards the structural modelling of the active site of ascorbate oxidase." Thesis, University of Nottingham, 2001. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.368242.
Full textSchmitt, Benoît. "5,6,7,8-tétrahydro-1,6-naphtyridines : dérivés et analogues structuraux." Université Louis Pasteur (Strasbourg) (1971-2008), 2004. http://www.theses.fr/2004STR13210.
Full textTruel, Isabelle. "Synthèses d'hétérocycles phosphoniques dans les séries de l'indole, du furane, du pyrrole et de la pyridazine." Rouen, 1998. http://www.theses.fr/1998ROUES062.
Full textMernari, Bouchaïb. "Complexes binucléaires de dérivés de la pyridazine ou du pyrazole synthèses, structures cristallines et interactions magnétiques /." Grenoble 2 : ANRT, 1987. http://catalogue.bnf.fr/ark:/12148/cb37607939k.
Full textHervet, Maud. "Réactions d'arylation et d'hétéroarylation métallo-catalysées en séries imidazo[1,2-α]pyridine et imidazo[1,2-β]pyridazine." Tours, 2002. http://www.theses.fr/2002TOUR3803.
Full textAs part of our on-going efforts to study the reactivity and pharmacological properties of bridgehead nitrogen heterocycles developped in our laboratory, we turned out our attention to new methods of arylation and heteroarylation reactions of imidazoazines. In order to realize this study, we investigated the metallo-catalyzed cross-coupling between aryl halides or sulfonates and organometallic compounds which constitute the most powerful C(sp²)-C(sp²) bond-forming reactions. We chose to study four cross-coupling reactions which are widely used in organic chemistry : Suzuki, Kumada, Negishi and Stille. In each case, the two possible ways of functionalization were investigated, from the halogenoimidazoazine or its corresponding organometallic derivative. Our initial forays was the investigation of reactivity of 3 and 6 positions of imidazo[1,2-α]pyridines and imidazo[1,2-β]pyridazines toward the Suzuki-type reaction. Then, each coupling method was applied on the 3 and 6 positions of imidazo[1,2-α]pyridine in order to establish optimal conditions of functionnalization
Moreau, Stéphane. "5-benzyl-6-methyl-pyridazines fonctionnalisees et systemes bicycliques condenses : syntheses, etudes pharmacologiques et modelisation moleculaire." Clermont-Ferrand 1, 1996. http://www.theses.fr/1996CLF1PP03.
Full textLe, Bourdonnec Bertrand. "Conception et synthèse de nouveaux ligands non peptidiques des récepteurs AT1 de l'angiotensine II." Lille 1, 1997. http://www.theses.fr/1997LIL10115.
Full textCONTRERAS, JEAN-MARIE. "Inhibiteurs reversibles de l'acetylcholinesterase et ligands des recepteurs muscariniques derives des 3-aminoalkyl-6-arylpyridazines (doctorat : pharmacochimie)." Strasbourg 1, 1999. http://www.theses.fr/1999STR15125.
Full textBains, Gurjeet Singh. "Cocoa flavour : the interaction of pyrazines with carboxylic acids." Thesis, Queensland University of Technology, 1995. https://eprints.qut.edu.au/36919/1/36919_Bains_1995.pdf.
Full textLandelle, Henriette. "Synthèse et étude physicochimique des pyridazino [4,5-b] carbazoles, benzofuro [3,2-f] phtalazines, pyrido [3', 4' : 4,5] furo [3,2-b] indoles, benzothiéno [2,3-g] cinnolines." Caen, 1988. http://www.theses.fr/1988CAEN4072.
Full textAchelle, Sylvain. "Synthèse de nouveaux oligomères possédant un ou plusieurs motifs diaziniques : applications en tant que cristaux liquides et matériaux fluorescents." Rouen, INSA, 2007. http://www.theses.fr/2007ISAM0012.
Full textAbou, Hamdan Hussein. "Synthèse de nouveaux agents anticancéreux." Thesis, Strasbourg, 2018. http://www.theses.fr/2018STRAF012.
Full textCancers represent a major public health problem hence the need to use new classes of medicines. Among the opportunities for developing new treatments, two have caught our attention and that of our collaborators: the modulation of splicing by compounds such as NVS-SM2, and the inhibition of the oncogene KRAS by derivatives of natural products, the flavaglines.In this context, we have developed the first robust synthesis of NVS-SM2, which can satisfy the global demand of this agent to examine in detail its therapeutic potential in different types of disorders. In addition, the synthetic strategy reported here could be extended to new analogues of this compound. Furthermore, we have synthesized new flavaglines that have been examined for their effects on KRAS inhibition. During this study, we discovered new reactions, including a dimethylcarbamoyl chloride-induced amine inversion of configuration
Salome, Christophe. "Construction de nouveaux hétérocycles par réaction de Buchwald : Synthèses et propriétés pharmacologiques." Université Louis Pasteur (Strasbourg) (1971-2008), 2007. http://www.theses.fr/2007STR13230.
Full textThe principal work of the Medicinal Chemist is the design and structural optimization of molecules of pharmacological and therapeutic interest. In this objective, we were interested in the modification of the molecular framework of known heterocyclic compounds and their pharmacological properties. Thus initially we developed new synthetic strategies for the construction of the general scaffold through the Buchwald reaction. The compounds were then pharmacologically evaluated in the search for new phosphodiesterase inhibitors. The adopted synthetic strategy implements a Buchwald reaction with an NH grouping which is slightly nucleophilic with strongly electron deficient halogenated heterocycles which generally results, after one or two additional stages, in novel, interesting heterocycles. By this method, a large number of novel heterocycles such as aza-benzodiazepin-2-ones, aza-benzodiazepine-2,5-diones, pyrido[4,5-b]imidazoles and the tricyclic systems of the benzopyridodiazepines type were synthesized successfully in a small number of steps. In the second objective, the impact of the structural modification (replacement of the heterocycle, the extension or the contraction of the ring system and the transformation of the bicyclic system into a tricyclic system) on the pharmacological properties and, in particular, on phosphodiesterase inhibition was studied. By modifying the structures, we also could more precisely include/understand the pharmacophore of this type of compounds. Among the number of analogues synthesized and tested some compounds have interesting phosphodiesterase-4 inhibitor properties
Conchon, Elizabeth. "Synthèse de nouveaux carbazoles inhibiteurs de la Chk1." Clermont-Ferrand 2, 2006. https://theses.hal.science/tel-00717338/document.
Full textParis, Antoine. "Synthèses de dérivés silylés en séries pyridinique et diazinique. Application de la réaction d'ipso-désilylation à l'élaboration de polyhétérocycles." Rouen, 1997. http://www.theses.fr/1997ROUES053.
Full textThomas, Jaron Michael. "On Metal synthesis of Some Substituted Rhenium and Manganese Complexes." TopSCHOLAR®, 2012. http://digitalcommons.wku.edu/theses/1225.
Full textAubé, Christophe. "Synthèse de nouveaux systèmes polyaza-hétérocycliques pyridaziniques et pyrroliques : nouvelles méthodologies de synthèse et application en chimie supramoléculaire." Nantes, 2012. http://archive.bu.univ-nantes.fr/pollux/show.action?id=effb683e-361f-4a47-b3b3-bb75fd3756f9.
Full textThe nitrogen heterocycles, pyridazine and pyrrole, are present in many molecules with interests in field such as biology (antifungal, anti-inflammatory, anticancer agents. . . ), electronic (organic transistors), supramolecular chemistry (self-organizing architectures like grid and helix) and organic catalysis. We first focused on the development of a new methodology for the synthesis of dissymmetrical 3,6-diaryl- and triheteroaryl-pyridazines involving the formation of two successive C-C bonds by the use of triaryl- and triheteroaryl-bismuths reagents. Then, biological tests will be conducted to assess their potential, particularly in oncology. The second part of our work concerns the synthesis of new polyaza-heteroaromatic compounds, based on pyridazinic and pyrrolic cycles, inserted in the middle of an oligoamidic sequence to form a helical foldamer, able to encapsulate substrates. The role of this ”central linker” is to modulate the volume of the foldamer cavity in order to trap molecules with different sizes. The strategies used for the synthesis of the linkers based on pyridazines pass through C-C cross-coupling reactions and those based on pyrrolic cycles involve an electrochemical reduction of pyridazines
Oudot, Romain. "Synthèse de dérivés imidazo[1,2-a] pyridines et imidazo[1,2-b] pyridazines tricycliques." Thesis, Tours, 2009. http://www.theses.fr/2009TOUR3804.
Full textThe imidazo[1,2-a]pyridines and imidazo[1,2-b]pyridazines moeities are very studied by scientific community, specially in therapeutic field. This is mostly due to recent progress in metallocatalyzed couplings which allow easier functionnalization of these structures. However, the tricyclic derivatives of these compounds remained not very studied despite important biological properties of some of there isosters. This thesis is divided in two parts : -The synthesis of imidazo[1,2-b]pyridazines with a dinitrogenated third cycle between the positions 7 and 8 in collaboration with Sanofi-Aventis. These new compounds were a real chemical challenge and their synthesis required important works of development. We used various metallocatalyzed couplings methods. -The synthesis of imidazo[1,2-a]pyridines with a pyridinic cycle between the positions 2 and 3. These molecules, poorly described in the literature, have never been subject to biological study. In order to effectively synthesize an interesting range of these structures, I have developed a new heterocyclization method which allows us to obtain in two steps, starting from commercialy available starting materials, some original tricyclics compounds
Scott, Joseph Brian. "Synthesis and Characterization of Some Rhenium Complexes." TopSCHOLAR®, 2009. http://digitalcommons.wku.edu/theses/114.
Full textGouault, Nicolas. "Mise au point de nouvelles méthodes de synthèse de lactones et de 4,5-dihydro-3(2h)-pyridazin-3-ones sur support solide : évaluation de leur activité biologique." Rennes 1, 2002. http://www.theses.fr/2002REN1A004.
Full textParrot, Isabelle. "Synthèse et étude pharmacologique d'agents cholinergiques promnésiques : Approche par la synthèse parallèle en phase solide, et développement de ligands fluorescents." Université Louis Pasteur (Strasbourg) (1971-2008), 2001. http://www.theses.fr/2001STR13201.
Full textMohamed-Hachi, Abdourahman. "Synthèse d'éthers de diénols phosphoniques et de leurs précurseurs carbonylés. Etude de leur réactivite dans des réactions de polyvinylogation et de cycloaddition [4+2]." Rouen, 1999. http://www.theses.fr/1999ROUES058.
Full textFogain-Ninkam, Alain. "Synthèse de structures hétérocycliques incluant un motif isoindole par cyclisation intramoléculaire." Le Havre, 2000. http://www.theses.fr/2000LEHA0007.
Full textHuynh, Thi Ngoc Phuong. "Synthèse et études des relations structure/activité quantitatives (QSAR/2D) d'analyse benzo[c]phénanthridiniques." Phd thesis, Université d'Angers, 2007. http://tel.archives-ouvertes.fr/tel-00346332.
Full textUne recherche de relation structure/activité quantitative (RSAQ/2D) a été menée. L'équation de RSAQ/2D a été construite à partir de 88 analogues de BZP possédant une activité antitopoisomérase en utilisant le logiciel MOE. Ces résultats sont exploités dans le cadre de la prédiction de cytotoxicité de nos nouvelles structures et pour orienter nos futurs travaux. Les valeurs prédictives montrent que l'activité biologique de ces composés dépend non seulement du groupement éthoxyle en position 12 mais également de la présence de deux atomes d'azote dans le cycle A.
Holm, Camala Sue. "Pyrazines and organic acids in cocoa : their analysis and effect on chocolate flavour." Thesis, Queensland University of Technology, 1991. https://eprints.qut.edu.au/35962/1/35962_Holm_1991.pdf.
Full textN'gompaza, Diarra Joannah. "Synthèse et évaluation biologique d’imidazo[1,2-b]pyridazines et de purines inhibitrices de protéines kinases." Thesis, Paris 5, 2012. http://www.theses.fr/2012PA05P613/document.
Full textThis thesis focuses on the synthesis and biological evaluation of new kinase inhibitors. Kinase deregulation is associated with numerous diseases such as cancer or neurodegenerative diseases. In the first part of this work, 2,6,9-trisubstituted purines bearing at C-2 position aminodiols derivatives were prepared. Aminodiols were obtained either via Sharpless asymmetric dihydroxylation or by reduction of amino esters. The compounds appeared to be more potent against kinases than (R)-roscovitine which is presently undergoing phase II clinical tests. In particular, inhibition of CK1, CDK5 and CDK9 were observed with IC50 < 200 nM. The compounds prepared showed an antiproliferative effect against tumor cell-lines (SH-SY5Y). Eventually, one of the most promising compounds was assayed against a series of cyt P450 enzymes and did not showed any inhibition (IC50 > 5 μM). The second family of compounds prepared in this work is imidazo[1,2-b]pyridazines. A new route to 3,6,8-trisubstituted imidazo[1,2-b]pyridazines was first developed. These products were shown to be highly potent inhibitors of several kinases such as CDK5 and CK1 (IC50 < 50 nM). The kinase inhibitions were accompanied by antiproliferative activities against tumor cell-lines. Finally, a series of 3,6-disubtituted imidazo[1,2-b]pyridazines was also prepared and appeared to be selective inhibitors of CLK1 (IC50 < 100 nM)
Mykhaylychenko, Sergiy. "Study of perfluoroketene dithioacetals and N,S-acetals for the synthesis of fluorinated acyclic and heterocyclic compounds." Rouen, 2008. http://www.theses.fr/2008ROUES066.
Full textPerfluoroketene dithioacetals are simple and highly versatile building-blocks for the synthesis of various fluorinated acyclic and heterocyclic compounds. Efficient and straightforward transformation of a,b-unsaturated g-lactones into 2,2,2-trifluoroethyl substituted γ-lactams and pyridazin-3-ones was performed, starting from a variety of primary amines or hydrazines and perfluoroketene dithioacetatals. The structures of all new compounds were ascribed using NMR (19F, 1H, 13C), IR, MS data and X-ray diffraction analysis. The possible mechanisms for the formation of γ-lactams and pyridazin-3-ones are also presented. The reactions of N-monosubstituted polyfluorothioamides with alkyllithium reagents were studied. In the case of N,N-disubstituted perfluorothioamides N,S-acetals were obtained. Some chemical properties of perfluoroketene-N,S-acetals, including oxidation and chlorination reactions, were investigated. Oxidation reaction of perfluoroketene-N,S-acetals with t-butylhydroperoxide led to a formation of a-hydroperfluoroamides. Chlorination of perfluoroketene-N,S-acetals with sulfuryl chloride gave a-chloroperfluoroamides; this method proved to be a new approach in the synthesis of polyfluorinated a-chloro optically active compounds. The possible mechanisms for these transformations are discussed
CHAMBON, JEAN-PIERRE. "Caracterisation de derives pyridazinyl-gaba comme ligands antagonistes du recepteur gaba-a." Université Louis Pasteur (Strasbourg) (1971-2008), 1987. http://www.theses.fr/1987STR13002.
Full textBelaroussi, Rabia. "Synthèse et fonctionnalisation de nouveaux dérivés tricycliques [6-5-6] polyhétéroaromatiques à visée thérapeutique potentielle." Thesis, Orléans, 2016. http://www.theses.fr/2016ORLE2002/document.
Full textThe discovery of new candidates to fight against various diseases, namely cancer and neurodegenerative diseases, is one of the main goals of our research group. In this context, the main purpose of this thesis, is the design of two new classes of heterocyclic planar structure, to date, rarely studied, namely pyrido[2’,1’ :1,5]pyrazolo[3,4-d]pyridazines and pyrido[2’,1’ :1,5]pyrazolo[3,4-d]pyrimidines. This manuscript is essentially dedicated to a methodology work describing the different routes of access to these originals and potentially modular tricyclic precursors. The reactivity of these key synthons is then studied towards aromatic nucleophilic substitutions reactions and various palladocatalyzed methods of functionalization (Suzuki-Miyaura, Buchwald-Hartwig, activation PyBrOP-(hetero) arylation) to develop interesting libraries built around these unusual structures, thus opening numerous pharmacologicals perspectives
Pollet, Pamela. "Métallation ortho-dirigée par des groupes sulfures en série diazinique. Synthèses de sulfoxydes chiraux et étude de l'induction asymétrique de ces groupes en série aromatique π-déficitaire." Rouen, 1998. http://www.theses.fr/1999ROUES028.
Full textRosa, Fernanda Andreia. "Acilenaminonas: Síntese e Aplicação na Obtenção de Pirazóis, Pirazolo[3,4-d]piridazinonas e Pirazolo[1,5-a]pirimidinas." Universidade Federal de Santa Maria, 2009. http://repositorio.ufsm.br/handle/1/4174.
Full textThe regioespecific synthesis of a series of 14 N-acylated enaminones (52-88%) from the acylation reaction of secondary β-enamino ketones [RC(O)CH=CHNR1R2; R = Ph, 4- FC6H4, 4-NO2C6H4, thien-2-yl, CCl3, CF3; R1 = H; R2 = Bn, Ph, 4-NO2C6H4] with trifluoroacetic anhydride or ethyl oxalyl chloride in pyridine is reported. On the other hand, when tertiary enaminone precursors [R = Ph, 4-MeC6H4, 4-MeOC6H4, 4-BrC6H4, 4-ClC6H4, 4-FC6H4, 4-O2NC6H4, thien-2-yl, benzofur-2-yl, CCl3, CF3; R1,R2 = Me] were used, the acylation reaction led to a series of 17 C-acylated enaminones (75-95%). A series of 4-substituted-1H-pyrazole-5-carboxylates (73-94%) were obtained regiospecifically from the cyclocondensation reaction of non symmetrical enaminodiketones [RC(O)C(=CHNMe2)C(O)CO2Et; R = Ph, 4-MeOC6H4, 4-ClC6H4, 4-FC6H4, 4-O2NC6H4, thien-2-yl, benzofur-2-yl, CCl3, CF3] with tert-butylhydrazine or carboxymethylhydrazine. The reaction of these pyrazole-5-carboxylates (R = 4-MeOC6H4, 4-FC6H4, benzofur-2-yl, CF3) with hydrazine lead to synthesis of 4- substituted-pyrazolo[3,4-d]pyridazinones (74-96%). In addition, the reaction of enaminodiketones (R = Ph, 4-MeC6H4, 4-MeOC6H4, 4-BrC6H4, 4-ClC6H4, 4-FC6H4, 4- O2NC6H4, thien-2-yl, benzofur-2-yl) with 3-amino-5-methylpyrazole was performed, where a series of pyrazolo[1,5-a]pyrimidine-7-carboxylates were obtained regiospecifically (53-79%).
A síntese de uma série de 14 enaminonas N-aciladas regioespecificamente (52-88%) foi realizada a partir da reação de acilação de enaminonas secundárias [RC(O)CH=CHNR1R2; R = Ph, 4-FC6H4, 4-NO2C6H4, tien-2-il, CCl3, CF3; R1 = H; R2 = Bn, Ph, 4-NO2C6H4] com anidrido trifluoracético e com cloreto de etil oxalila em piridina. Quando foram utilizados como precursores enaminonas terciárias [R = Ph, 4-MeC6H4, 4-MeOC6H4, 4-BrC6H4, 4-ClC6H4, 4-FC6H4, 4-O2NC6H4, tien-2-il, benzofur-2-il, CCl3, CF3; R1,R2 = Me] a reação de acilação levou à obtenção regioespecífica de 17 enaminonas C-aciladas (75-95%). Uma série de 5-carboxietil-1H-pirazol 4-substituídos foi obtida regioespecificamente (73-94%) a partir da ciclocondensação das enaminodicetonas não simétricas [RC(O)C(=CHNMe2)C(O)CO2Et; R = Ph, 4-MeOC6H4, 4-ClC6H4, 4-FC6H4, 4-O2NC6H4, tien-2-il, benzofur-2-il, CCl3, CF3] com tert-butilidrazina ou carboximetilidrazina. A reação destes pirazóis (R = 4-MeOC6H4, 4-FC6H4, benzofur-2-il, CF3) com hidrazina monoidrato levou à síntese de pirazolo[3,4-d]piridazinona 4- substituídas (74-96%). Também foi realizada a reação de ciclocondensação de enaminodicetonas (R = Ph, 4-MeC6H4, 4-MeOC6H4, 4-BrC6H4, 4-ClC6H4, 4-FC6H4, 4-O2NC6H4, tien-2-il, benzofur-2-il) com 3-amino-5-metilpirazol onde as 7-carboxietilpirazolo[1,5-a]pirimidinas 6-substituídas foram obtidas regioespecificamente (53-79%).
Ndzi, Bruno. "Métallation de pyrazines et de pyridazines : application à la synthèse de molécules actives. Nouvelle voie d'accès à des acides pyridinecarboxyliques." Rouen, 1994. http://www.theses.fr/1994ROUES015.
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