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1

Berg, Michael Arthur George. "Studies in the stereoselective synthesis of 1,1-disubstituted 1,2,3,4-tetrahydroisoquinolines." Diss., This resource online, 1992. http://scholar.lib.vt.edu/theses/available/etd-10032007-171522/.

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2

Jones, Michael William Chemistry Faculty of Science UNSW. "Enhancing the cooperative binding properties of 1,1'-bis(1,2,3,4-tetrahydroisoquinolines)." Awarded by:University of New South Wales. School of Chemistry, 2005. http://handle.unsw.edu.au/1959.4/27400.

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The design of partially reduced 1,1'-bisisoquinoline derivatives was investigated with the aim of controlling the conformation about the C1-C1' axis. This would produce ligands with unusual but predictable ligand binding properties, particularly cooperativity. The introduction of ??-aminoalkyl, ??-azidoalkyl, ??-alkynyl and ??-alkenyl groups onto the nitrogens of the reduced bisisoquinoline core was conducted with the intention of broadening the scope of the ligand. Subsequent epoxidation, hydroboration and Huisgen 1,3-dipolar cycloaddition of terminal unsaturated groups and nucleophilic displ
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3

Donaghy, Michael. "Studies in benzimidazo [2,1-a] isoquinoline chemistry." Thesis, Northumbria University, 2001. http://nrl.northumbria.ac.uk/1217/.

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Studies in Benzimidazo[2,1-a]isoquinoline Chemistry by Michael John Donaghy B. Sc. (Hons.) Ellipticine, a member of the pyrido[4,3-b]carbazole alkaloid family first isolated in 1959 from the leaves of the plant Ochrosia Elliptica has been shown to possess anti-cancer activity against various tumours. Ellipticine is thought to undergo biological oxidation to give the more active 9-hydroxyellipticine that is subsequently converted to a highly reactive quinone-imine intermediate. The quinone-imine is then thought to interact with bionucleophiles in the body promoting cell death. The aim of the pr
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4

Clifton, Mary Jennifer. "Studies in stereoselective synthesis via reissert compound chemistry." Thesis, This resource online, 1991. http://scholar.lib.vt.edu/theses/available/etd-08222009-040256/.

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5

Guimond, Nicolas. "Part A: Rhodium-catalyzed Synthesis of Heterocycles / Part B: Mechanistic Studies on Tethering Organocatalysis Applied to Cope-type Alkene Hydroamination." Thèse, Université d'Ottawa / University of Ottawa, 2012. http://hdl.handle.net/10393/23222.

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The last decade has been marked by a large increase of demand for green chemistry processes. Consequently, chemists have focused their efforts on the development of more direct routes toward different classes of targets. In that regard catalysis has played a crucial role at enabling key bond formations that were otherwise inaccessible or very energy and resources consuming. The central theme of this body of work concerns the formation of C–N bonds, either through transition metal catalysis or organocatalysis. These structural units being highly recurrent in biologically active molecules, the e
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6

Ford, Alan John. "Synthesis of substituted isoquinoline ligands for homogeneous catalysis." Thesis, University of Hull, 1996. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.361496.

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7

Muzanila, Charles Nobert. "Heterocyclic transformations involving #DELTA#'2-oxazolines and 1,2-benzisoxazoles." Thesis, University of Salford, 1989. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.327958.

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8

Hamilton, Lynne. "Synthesis, stereochemistry and reactions of quinoline, isoquinoline and acridine metabolites." Thesis, Queen's University Belfast, 1991. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.334710.

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9

Streetley, Guy Bradwell. "New approaches for the asymmetric synthesis of pyrroloisoquinoline and isoquinoline alkaloids." Thesis, Loughborough University, 2006. https://dspace.lboro.ac.uk/2134/34917.

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Pyrroloisoquinoline (n = 1) and the pyridoisoquinoline (n = 2) ring systems (2) are found to be the major structural motif of the Erythrina and the protoberberine group of alkaloids, respectively. We have recognised that suitable bicyclic lactams (1) could act as precursors, in an intramolecular N-acyliminium ion-mediated cyclisation, resulting in a stereoselective approach to the core of the Erythrina and protoberberine ring systems. [Illustration omitted.] Access to the tetracyclic core of the Erythrina alkaloids (3) through the application of N-acyliminium ion chemistry is well established
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10

Chow, Yit Lai. "Caenorhabditis elegans as a whole organism screening system for isoquinoline alkaloid bioactivities." 京都大学 (Kyoto University), 2014. http://hdl.handle.net/2433/188834.

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11

Sampaio, Tuane Bazanella. "AVALIAÇÃO DOS EFEITOS FARMACOLÓGICO E TOXICOLÓGICO DE 4- ORGANOCALCOGENO-ISOQUINOLINAS." Universidade Federal de Santa Maria, 2014. http://repositorio.ufsm.br/handle/1/11226.

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Coordenação de Aperfeiçoamento de Pessoal de Nível Superior<br>Monoamine oxidase (MAO) is a target enzyme in the treatment of several pathologies, being that new molecules which inhibit of a selective, potent and reversible manner their isoforms and without adverse effects are searched. In this way, the first manuscript of this dissertation evaluated the in vitro inhibitory potential of the 4-organochalcogen-isoquinolines on cerebral MAO-A and B activities, elucidating their kinetics profile and the interaction compound x enzyme. The results demonstrated that all compounds were selective
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12

Morishige, Takashi. "Molecular characterization of O-methyltransferases involved in isoquinoline alkaloid biosynthesis in Coptis japonica." Kyoto University, 2002. http://hdl.handle.net/2433/149491.

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Kyoto University (京都大学)<br>0048<br>新制・課程博士<br>博士(農学)<br>甲第9734号<br>農博第1283号<br>新制||農||850(附属図書館)<br>学位論文||H14||N3697(農学部図書室)<br>UT51-2002-J516<br>京都大学大学院農学研究科応用生命科学専攻<br>(主査)教授 佐藤 文彦, 教授 關谷 次郎, 教授 島田 幹夫<br>学位規則第4条第1項該当
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13

Shitan, Nobukazu. "Structural and functional analyses of an ABC protein in isoquinoline alkloid-producing plant cells." Kyoto University, 2003. http://hdl.handle.net/2433/78151.

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Kyoto University (京都大学)<br>0048<br>新制・課程博士<br>博士(農学)<br>甲第10251号<br>農博第1323号<br>新制||農||865(附属図書館)<br>学位論文||H15||N3772(農学部図書室)<br>UT51-2003-H672<br>京都大学大学院農学研究科応用生命科学専攻<br>(主査)教授 佐藤 文彦, 教授 關谷 次郎, 教授 矢崎 一史<br>学位規則第4条第1項該当
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14

Si, Chong. "Synthesis of Cortistatin Alkaloids and a Versatile Synthesis of Isoquinolines." Thesis, Harvard University, 2012. http://dissertations.umi.com/gsas.harvard:10444.

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The cortistatins are a recently identified class of marine natural products that were found to exhibit potent and selective inhibition of human umbilical vein endothelial cells (HUVECs), making them promising leads for the development of anti-angiogenic drugs. In our synthesis, we envisioned that natural cortistatins and unnatural analogs could be prepared by late-stage introduction of isoquinolines to 17-keto precursors, and that these differentially substituted precursors could all be derived from a common key intermediate 112. We developed a robust synthetic route to prepare gram quantities
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15

Xu, Yiting. "Identification of [beta]-carboline/isoquinoline biosynthetic enzymes from brain tissue and characterisation of mupirocin biosynthetic proteins." Thesis, University of Bristol, 2008. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.506563.

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16

Tittle, James Alfred. "Ab Initio Studies of High Temperature Pyrolysis Mechanisms in Heterocyclic Nitrogen-Containing Compounds." Digital Commons @ East Tennessee State University, 2000. https://dc.etsu.edu/etd/21.

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The decomposition mechanisms of various coal constituents undergoing pyrolysis are of great concern in environmental circles (especially those coal constituents containing nitrogen). Most methods of burning coal that are efficient involve doing so at high temperatures. This invariably results in a large portion of non-combusting coal being heated to high temperatures also causing pyrolysis of the original coal constituents. The end result of such pyrolysis is the production of a number of noxious gaseous products. If we are to design methods of reducing the amount of toxins that are produced f
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17

Smith, Catherine Claire. "The mouse tail model in dermatology : a histological study on the effects of crude coal tar and isoquinoline." Thesis, University of Cambridge, 1987. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.236062.

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This study involves a morphological and histological investigation of normal mouse tail skin and its response to crude coal tar and isoquinoline (a major constituent of coal tar). Mouse tail skin is unusual in that it undergoes both parakeratotic and orthokeratotic keratinization in adjacent sites. The former develops without a granular layer and resembles psoriasis, while the latter, with a granular layer, resembles normal human skin. Based on this property, mouse tail skin has frequently been used as a model for psoriasis but in spite of this, an integrated, detailed picture of its structure
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18

Tims, Michael C. "The chemical ecology of Hydrastis canadensis L. (Ranunculaceae) effects of root isoquinoline alkaloids on the Hydrastis endophyte, Fusarium oxysporum /." College Park, Md. : University of Maryland, 2006. http://hdl.handle.net/1903/4052.

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Thesis (Ph. D.) -- University of Maryland, College Park, 2006.<br>Thesis research directed by: Cell Biology & Molecular Genetics. Title from t.p. of PDF. Includes bibliographical references. Published by UMI Dissertation Services, Ann Arbor, Mich. Also available in paper.
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19

McNaught, Kevin St Patrick. "The neurotoxic potential of isoquinoline derivatives structurally related to the Parkinsonism-inducing neurotoxin 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine." Thesis, King's College London (University of London), 1996. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.321681.

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20

Pulman, Jane. "A transcriptomics approach to understanding polymorphic and transcript level differences linked to isoquinoline alkaloid production in triploid varieties of Narcissus pseudonarcissus." Thesis, University of Liverpool, 2014. http://livrepository.liverpool.ac.uk/2006379/.

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The Amaryllidaceae have characteristic isoquinoline alkaloids including galanthamine that is approved for treatment of Alzheimer’s disease. The daffodil (Narcissus pseudonarcissus) is an industrial source of this alkaloid. This project undertook analysis of the daffodil transcriptome as an approach to understanding this alkaloid biosynthetic pathway. Material from the basal plate of var. Carlton was analysed using the Roche 454 GS FLX Titanium and Illumina HiSeq platforms to assemble reference transcripts (45324 transcripts from 454, 165065 from Illumina). Annotation was via a bespoke BLAST pi
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21

Pesarico, Ana Paula. "ENVOLVIMENTO DOS SISTEMAS SEROTONINÉRGICO E DOPAMINÉRGICO NA AÇÃO DO TIPO ANTIDEPRESSIVA DO 7-FLÚOR-1,3 DIFENILISOQUINOLINA-1-AMINO EM CAMUNDONGOS." Universidade Federal de Santa Maria, 2014. http://repositorio.ufsm.br/handle/1/11237.

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Coordenação de Aperfeiçoamento de Pessoal de Nível Superior<br>Depression is a psychiatric disorder associated with a negative impact on quality of life. Monoaminergic system has been involved in this disease and in the action of antidepressants. This study aimed to investigate the potential antidepressant-like of 7-fluoro-1,3-diphenylisoquinoline-1-amine (FDPI) and the possible involvement of monoaminergic system. Results showed that FDPI (1, 10 and 20 mg/kg, intragastric (i.g.)) reduced the immobility time, increased swimming time, but did not alter climbing time of mice in the modified forc
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22

Ozcan, Sevil. "Development Of New Synthetic Methodologies For The Synthesis Of Unusual Isocoumarin And Indole Derivatives:the Chemistry Of Homophthalic Acid." Phd thesis, METU, 2007. http://etd.lib.metu.edu.tr/upload/3/12608197/index.pdf.

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Many heterocyclic compounds containing nitrogen, oxygen and sulfur show wide range of physiological activities and their synthesis has always been attracted the interest of chemists. The aim of this research is to develop new synthetic methodologies leading to the synthesis of new derivatives of isocoumarines, indoles, isoquinolines, benzodiazepinones and quinazolines, which have been found to show important biological activities. Starting from homophthalic acid and bishomophthalic acid the corresponding acyl azides were proposed to be synthesized, which then would be used for the synthesis of
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23

Charpentier, Langlois Patricia. "Activation d'une réaction entre un acide et une amine par reconnaissance moléculaire. Synthèse d'un récepteur d'amine." Rouen, 1995. http://www.theses.fr/1995ROUES027.

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Notre objectif a été de définir un récepteur hétérocyclique susceptible de faciliter, de manière générale, la réaction entre un acide carboxylique et une amine afin de conduire à un amide. La première partie de ce travail a consisté en l'examen de diverses stratégies d'approche de la partie tricyclique du récepteur. Nous nous sommes notamment intéressés à des dérivés de la tétrahydroisoquinoléine. A cette occasion, nous avons été amenés à apporter une contribution intéressante à la chimie de ce type de dérivés. Dans une seconde partie, nous nous sommes attachés à synthétiser la partie simplifi
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24

Tinkleman, Joseph M. Smith Forrest T. "Synthesis of 10, 11, 12, 12a, 12b, 13-hexahydro-5hbenzo[f]cyclopropa[d]pyrido[1,2-b] isoquinoline-5,7(9H)dione and related compounds." Auburn, Ala, 2009. http://hdl.handle.net/10415/1655.

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25

Laughlin, Sarah R. "Arylboronic Acids With Strong Fluorescence Intensity Changes Upon Sugar Binding." Digital Archive @ GSU, 2011. http://digitalarchive.gsu.edu/chemistry_theses/46.

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Boronic acids play an important role in the design and synthesis of chemosensors for carbohydrates due to their ability to reversibly bind with diol-containing compounds. Along this line, the availability of boronic acids that change fluorescence upon sugar binding is critical to a successful sensor design effort. Here, two boronic acids that show strong fluorescent intensity changes upon sugar binding are reported: isoquinoline-7-boronic acid (7-IQBA) and phenoxathiin-4-boronic acid (4-POBA).
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26

Müller, Thomas. "C-H Activation by Nickel and Iron Catalysis." Doctoral thesis, Niedersächsische Staats- und Universitätsbibliothek Göttingen, 2019. http://hdl.handle.net/21.11130/00-1735-0000-0003-C189-8.

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27

Brine, Natalie Dawn. "Investigation of the phytochemistry and biological activity of isoquinoline alkaloids isolated from the South African medicinal plants, cyrtanthus sanguineus (Lindl.) walp. and cyrtanthus obliquus (L.f.)ait." Doctoral thesis, University of Cape Town, 2001. http://hdl.handle.net/11427/3274.

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Bibliography: p. 128-140.<br>The term "traditional medicine" refers to the ways of protecting and restoring health that existed before the arrival of modern medicine. These approaches to health belong to the traditions of each country and have been handed down from generatio to generation.
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28

Hedouin, Jonathan. "Etude de cascades réactionnelles pallado-catalysées de fermeture d’allènamides et d’allylation directe de liaisons C-H et C-CO2H d’azoles, d’énamides et d’acides propioliques pour la diversité structurelle." Thesis, Normandie, 2017. http://www.theses.fr/2017NORMIR21/document.

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Le développement de plans synthétiques de molécules de complexité variable qui utilise des réactifs aisés d’accès et qui sont économes en atomes et en étapes est constamment au cœur des préoccupations du chimiste organicien pour accroître la diversité moléculaire de façon efficace et éco-responsable. La catalyse par les métaux de transition a permis de faire des progrès considérables dans la construction et la fonctionnalisation combinées d’hétérocycles d’intérêt à valeur ajoutée dans les sciences des produits naturels et les industries pharmaceutiques et phytosanitaires. Le principe synthétiq
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29

Carvalho, Kaline Rodrigues. "Bioactive alkaloids and phenolic Hippeastrum solandriflorum (Lindl.) - Amaryllidaceae." Universidade Federal do CearÃ, 2014. http://www.teses.ufc.br/tde_busca/arquivo.php?codArquivo=13544.

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This work describes the phytochemical study of Hippeastrum solandriflorum(Amaryllidaceae)aiming the isolation and structural elucidation of new bioactive compounds, as well as its pharmacological investigation. The chemical investigation realized with the EtOH extract from bulbs, through chromatographic methods, including HPLC (reverse phase), resulting inthe isolation of ten compounds: a furan derivative: 5-(hydroxymethyl)furan-2-carbaldehyde(HS-1), two phenolic derivatives: piscidic acid (HS-2), eucomic acid (HS-3), and seven isoquinoline alkaloids: narciclasin ( HS-4), 2&#945;-hydroxypseudo
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30

Rinaldi, Maria Valeria Nani. "Avaliação da atividade antibacteriana e citotóxica dos alcalóides isoquinolínicos de Annona hypoglauca Mart." Universidade de São Paulo, 2007. http://www.teses.usp.br/teses/disponiveis/9/9138/tde-28032008-134727/.

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Annona hypoglauca Mart. foi coletada em área inundada da Floresta Amazônica, próximo à Manaus (Brasil). Os alcalóides foram obtidos do extrato bruto do caule por partição ácido-base, e a partir do resíduo dessa extração foi realizada a partição com solventes de diferentes polaridades, originando as frações livres de alcalóides. A partir da análise de CG-EM dos alcalóides totais foi possível caracterizar sete alcalóides aporfínicos (actinodafinina, anonaina, glaucina, isoboldina, isodomesticina, nornuciferina e roemerina) e possivelmente duas protoberberinas (esculerina e caseadina). Os alcalói
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31

Siqueira, Carlos Alberto Theodoro. "Aspectos químicos e atividade antiprotozoária in vitro de Annona coriacea Mart. (Annonaceae)." Universidade de São Paulo, 2010. http://www.teses.usp.br/teses/disponiveis/9/9138/tde-31012011-140840/.

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Estudos anteriores dos alcalóides totais (AT) de Annona coriacea Mart. (Annonaceae) revelaram atividade antiprotozoária promissora. No presente trabalho, realizou-se o fracionamento biomonitorado dos AT de folha e selecionaram-se duas frações ativas (100% morte), frente às formas promastigotas de Leishmania (L.) chagasi in vitro, para a caracterização dos alcalóides, por CG-EM. Os AT bioativos de caule (100% morte) foram analisados sem fracionamento prévio. Em paralelo, efetuou-se amostragem de três exemplares de A. coriacea, analisados em conjunto, para o acompanhamento da variação do rendime
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32

Bender, Christoph. "Stereoselektive Synthese neuartiger 1,2-Dihydroisochinoline als Vorstufen für die Alkaloidsynthese." Doctoral thesis, Humboldt-Universität zu Berlin, Mathematisch-Naturwissenschaftliche Fakultät I, 2008. http://dx.doi.org/10.18452/15728.

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Ausgangspunkte der vorliegenden Arbeit waren stereoselektive Synthesen von Reissert-Verbindungen über chirale N-Acylisochinoliniumsalze. Es galt die Konfiguration der erhaltenen Produkte zu beweisen und deren Synthesepotential zu erforschen. Ein Ziel dieser Arbeit war es, weiterführende Reaktionen für die Synthese von alkaloidanalogen Substanzen zu entwickeln. Es gelang, die Reissert-Reaktion mit Chlorameisensäurementhylester erfolgreich auf andere Heterocyclen als Isochinolin auszudehnen. Die Annahme eine stereoselektiven Verlaufes mußte korrigiert werden. Das Reissert-Produkt konnte mit eine
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33

Pilgrim, Ben Samuel. "Novel palladium-catalysed routes to aromatic heterocycles." Thesis, University of Oxford, 2013. http://ora.ox.ac.uk/objects/uuid:d143b5bf-1738-48ce-be75-4a25249acb9d.

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A brief summary of the use of palladium as a catalyst, the characteristic reactivity of palladium complexes and the commonly used palladium-catalysed cross coupling reactions is given, with a special focus on the palladium-catalysed α-arylation of enolates and its application to the synthesis of aromatic heterocycles. The synthesis of aromatic heterocycles via both traditional methods and more recent metal-catalysed approaches is discussed in the context of isoquinolines. The palladium-catalysed oxidation of dihydrofurans bearing an ortho-bromophenyl group at the 2-position to the correspondin
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34

Blumenthal, Haiko. "Struktur und Reaktivität ausgewählter chiraler N-Acylaminohydroperoxide und -peroxide." Doctoral thesis, Humboldt-Universität zu Berlin, Mathematisch-Naturwissenschaftliche Fakultät I, 2009. http://dx.doi.org/10.18452/15868.

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Ausgangspunkte der vorliegenden Arbeit waren stereoselektive Synthesen von Reissert-analogen N-Acylaminohydroperoxiden über chirale N-Acylisochinoliniumsalze. Edukte waren Isochinolin(derivaten), Menthylchloroformiat und Wasserstoffperoxid. Es galt die Konfiguration der erhaltenen Produkte zu beweisen und deren Sauerstoffübertragungspotential zu erforschen. Ein zweites Ziel dieser Arbeit war es, von bekannten Diketopiperazinhydroperoxiden ebenfalls das Sauerstoffübertragungspotential zu überprüfen, weil sie die gleiche N-Acylaminohydroperoxidstruktur aufweisen aber bisher wenig untersucht wurd
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35

Santos, Maria de Fátima Costa. "Estudo fitoquímico e investigação da atividade citotóxica das folhas e cascas do caule de Guatteria pogonopus (Annonaceae)." Universidade Federal de Sergipe, 2015. https://ri.ufs.br/handle/riufs/6090.

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Coordenação de Aperfeiçoamento de Pessoal de Nível Superior<br>This paper presents the results obtained of the phytochemical bioguide of methanol extracts of the leaves and stem bark of Guatteria pogonopus Mart., a species belonging to the family Annonaceae. The botanical material (leaves and stem bark) were collected in the National Park Serra de Itabaiana (PARNA), Sergipe, Brazil. The extracts were obtained by maceration method at room temperature initially with hexane and then methanol, resulting in the hexane (EHF e EHC) and methanol (EMF e EMC) extracts, respectively. The methanol extr
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36

Gavin, James Patrick. "Control of regiospecificity in the synthesis of isoquinolines." Thesis, University of Manchester, 1989. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.252895.

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37

Sutton, Benjamin Josiah. "Intramolecular radical additions to pyridines, quinolines and isoquinolines." Thesis, University of Southampton, 2003. https://eprints.soton.ac.uk/426728/.

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38

Majeed, Amera Jihad. "Electrochemical oxidation of isochromanones, isoquinolines and related structures." Thesis, University of Bath, 1986. https://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.332114.

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39

Gatland, Alice Elizabeth. "Palladium-catalysed enolate arylation in the synthesis of isoquinolines." Thesis, University of Oxford, 2014. http://ora.ox.ac.uk/objects/uuid:f106760d-2375-4d56-81b2-faa6ee96cabc.

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<strong>Chapter 1. Introduction</strong> Scientific background on the development of homogeneous palladium-catalysed cross coupling reactions, focusing on the &alpha;-arylation reaction of enolates and its application to the synthesis of heteroaromatic compounds. The classical syntheses of isoquinolines are discussed, followed by an account of modern methods for their synthesis, including the recent &alpha;-arylation-based methodology developed by the Donohoe group. <strong>Chapter 2. Results and Discussion</strong> 2.1 Studies towards the development of a palladium-catalysed, C–H activation-b
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40

Berk, Mujde. "Development Of New Synthetic Methodologies For Isoquinolone And Isoindolinone Derivatives." Master's thesis, METU, 2010. http://etd.lib.metu.edu.tr/upload/3/12612145/index.pdf.

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ABSTRACT DEVELOPMENT OF NEW SYNTHETIC METHODOLOGIES FOR ISOQUINOLONE AND ISOINDOLINONE DERIVATIVES M&uuml<br>jde, Berk M.Sc., Department of Chemistry Supervisor: Prof. Dr. Metin Balci July 2010, 146 pages Due to the wide range of physiological activities, heterocycles containing nitrogen and oxygen have always attracted the interest of chemists. The objective of this research is to develop new synthetic routes to the synthesis of isoquinolone and isoindolinone derivatives starting from 2-(2-carboxyethyl)benzoic acid and homophthalic acid, respectively. The half ester produced from 2-(2-carboxy
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41

Brière, Jean-François. "Elaboration d'une enzyme artificielle se liant à des fonctions amines et des fonctions acides dans le but de catalyser la formation de liaisons amides." Rouen, 1998. http://www.theses.fr/1998ROUES097.

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Ce travail décrit l'élaboration d'un catalyseur supramoléculaire de structure hétérocyclique devant accélérer la formation de liaisons amides, en mimant les mécanismes enzymatiques. Une première synthèse à partir de la 4-amino-3-bromoisoquinoléine a ouvert deux nouvelles voies d'accès aux 2-méthyloxazolo[5,4-c]isoquinoléine et 1H-pyrrolo[3,2-c]isoquinoléine. Cette dernière structure a été fonctionnalisée en position 2 à l'aide d'une réaction de métallation. Au cours de la deuxième voie de synthèse nous avons établi l'influence de la substitution de la fonction amine d'aminopyrrolidine-2,5-dion
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42

Rathelot, Pascal. "Etude de la réactivité dans des réactions de transfert monoélectronique de nouveaux synthons isoquinoléiques à potentialités pharmacologiques." Aix-Marseille 3, 1995. http://www.theses.fr/1995AIX30005.

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Notre travail est consacre a l'etude de reactions par transfert monoelectronique en serie 5-nitroisoquinoleine. Nous avons dans un premier temps synthetise la 1-chloromethyl 5-nitroisoquinoleine dont l'etude de la reaction avec l'anion du 2-nitropropane a permis de conclure qu'elle se deroulait selon un mecanisme de substitution radicalaire nucleophile unimoleculaire (srn1). Cette reaction a ensuite pu etre generalisee a divers anions nitronate aliphatiques, cycliques et heterocycliques. Pour completer cette etude, la synthese de la 1-dichloromethyl 5-nitroisoquinoleine a ete realisee. L'etude
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43

Mimoun, Liliane. "Synthèse de nitriles chiraux via une catalyse duale et nouvelle méthodologie de synthèse d'isoquinoléines." Electronic Thesis or Diss., Orléans, 2024. http://www.theses.fr/2024ORLE1009.

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Nous avons développé une nouvelle approche via la catalyse duale permettant une activation orthogonale de chacun des deux partenaires organométalliques de couplage Pd/Cu afin de réaliser les réactions dans des conditions douces. Nous avons ainsi étudié la réaction d'α-allylation asymétrique de nitrile tertiaire en tirant profit d'une part du potentiel synthétique des céténimines N-métallées (M = Si, Cu) en tant que nucléophiles et d'autre part, de complexes α-allyl chiraux de palladium, en tant que partenaires électrophiles. Les céténimines N-métallés sont douées d'une chiralité planaire intri
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44

Berthault-Balâtre, Aurélie. "Synthèse et évaluation pharmacologique de ligands sélectifs du récepteur humain de l'Urotensine II." Orléans, 2005. http://www.theses.fr/2005ORLE2026.

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L'Urotensine II est un neuropeptide cyclique, initialement isolé chez les poissons téléostéens. Il est constitué par un enchaînement de 11 acides aminés avec une partie C-terminale hexacyclique, responsable de l'activité biologique. Ce système Urotensine II / UT est localisé dans différents tissus cardiovasculaires humains. Des effets puissants (vasoconstriction, prolifération vasculaire. . . ) ont été rapportés dans diverses espèces ainsi que chez l'Homme, suggérant la participation possible du système urotensinergique dans la physiopathologie cardiovasculaire. Dans la première partie de ce t
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45

Daras, Etienne. "Synthèse et évaluation biologique d’analogues aza de la combrétastatine A-4 comme inhibiteurs de la polymérisation de la tubuline." Aix-Marseille 1, 2008. http://www.theses.fr/2008AIX11079.

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Plusieurs séries de dérivés quinoléiques, isoquinoléiques et néoflavonoiques ont été préparées via une réaction clé de couplage de Suzuki, ou par cyclisation intramoléculaire de type Bischler-Napieralski. Des études de prolifération cellulaire ont mis en évidence des activités remarquables pour les composés de type 4-arylquinoléique et 4-indolylcoumarinique. Cette activité antiproliférative a été corrélée à une activité inhibitrice de l'assemblage de la tubuline. La nature et la position des substituants sur le cycle A n'influencent que très finement cette activité. Dans la série des dérivés n
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46

Stein, André Luiz Agnes. "Síntese de Calcogenofenos e Isoquinolinas via Reações de Ciclização Intramolecular." Universidade Federal de Santa Maria, 2013. http://repositorio.ufsm.br/handle/1/4254.

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Coordenação de Aperfeiçoamento de Pessoal de Nível Superior<br>In the first part of this work, a series of selenophenes and tellurophenes were prepared starting from of (Z)-chalcogenoenynes, by employing FeCl3 diorganyl dichalcogenide-mediated intramolecular cyclization. In general, the cyclic products were obtained in moderate to good yields. In order to evaluate the versatility of the obtained 3-chalcogen selenophene derivatives, we tested the reactivity of these compounds toward halogenation and Li/Se exchange reactions. In this way, the reaction of 2,5-diphenil-3-(fenilselene)-selenofene w
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47

Chiurato, Matteo. "Synthèse de tétrahydropyrido-[isoindolones/isoquinolones/indolizinones] pour l'élaboration d'inhibiteurs de CDks." Orléans, 2007. http://www.theses.fr/2007ORLE2069.

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Cette thèse est divisée en cinq parties. La première partie traite de la chimie des ions iminiums. Après une brève introduction sur leur découverte, sont présentées leurs préparations et leurs applications dans divers champs de la chimie, en particulier dans la synthèse de produits naturels. En suite nous traiterons des ions N-acyl iminiums, en évoquant les mécanismes de leur formation, les diverses applications et leurs particularités. La première partie se termine par la présentation des différentes voies d'accès à des structures du type isoindoquinolinonique obtenues notamment par formation
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48

Robveille, Jacques. "Synthèse de pyridine et d'isoquinoléine marquées au 14C sur l'hétérocycle azoté." Lyon 1, 1985. http://www.theses.fr/1985LYO10513.

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Trois procedes de synthese differents : la pyridine et les pyridines mono-2 et disubstituees-2,6 marquees c14 sont preparees a partir de composes marques dioxo-1,5 par cyclisation de leurs dioximes ; les pyridines substituees en 3 marquees c14 sont preparees par cyclisation thermique d'isocyanates de butadienyle prepares a partir des acides pentadiene-2,4oiques marques c14 ; les furo-, thieno- et pyrrolo (3,2-c) pyridines marquees c14 sont preparees a partir des acides furanne-, thiophene- et pyrroleacryliques-2 marques via les isocyanates. Application a la synthese d'isoquinoleines marques c1
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49

Gerfaud, Thibaud. "Nouvelles réactions d'hétéroannélation palladocatalysées à partir d'acyloximesSynthèse totale de l'alstoscholarine." Paris 11, 2010. http://www.theses.fr/2010PA112210.

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Ce manuscrit est consacré au développement de nouvelles réactions d'hétéroannélation palladocatalysées et à leur utilisation en synthèse totale. La première partie de ce manuscrit est dédiée au développement de nouvelles voies d'accès aux phénantridines, aux isoquinoléines, aux oxadiazolones et aux benzimidazoles à partir de dérivés d'oximes. Nous avons développé une nouvelle voie d'accès palladocatalysée aux phénantridines et aux isoquinoléines en utilisant une séquence domino aminopalladation/arylation directe. Cette approche est nouvelle et originale, car elle est basée sur l'insertion du p
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50

Eriksson, Ludvig. "Transition Metal Mediated Transformations of Carboranes." Doctoral thesis, Uppsala University, Organic Chemistry, 2003. http://urn.kb.se/resolve?urn=urn:nbn:se:uu:diva-3324.

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<p>This thesis describes the use of copper and palladium to mediate transformations of carboranes, especially <i>p</i>-carborane.</p><p>1-(1-<i>p</i>-carboranyl)-<i>N</i>-methyl-<i>N</i>-(2-butyl)-3-isoquinolinecarboxamide, a carborane containing analogue of the peripheral benzodiazepine receptor (PBR) ligand PK11195, has been synthesised. A key step in the reaction is the copper (I) mediated coupling of p-carborane with ethyl 1-bromo-isoquinoline-3-carboxylate. </p><p><i>p</i>-Carborane has been arylated on the 2-<i>B</i>-atom in high yields, using the Suzuki–Miyaura reaction. Thus the reacti
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