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1
Engqvist, Robert. "Syntheses of some tri- and tetracyclic heterocycles containing an indole moiety /." Stockholm, 2004. http://diss.kib.ki.se/2004/91-7140-161-X/.
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Somphol, Kittiya Chemistry Faculty of Science UNSW. "Synthesis of new heterocyclic structures based on indoles." Awarded by:University of New South Wales. Chemistry, 2007. http://handle.unsw.edu.au/1959.4/40829.
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Novel indolo-macrocycles have been generated from the attempts to synthesise bis-indolo-cyclotriveratrylenes by the condensation of I, I'-diindolyl-3,3'-dimethanols catalysed by p-toluenesulfonic acid. The addition of substituents on indoles led to enhanced solubilities of the macrocycles. Nine- and six-membered ring compounds have been synthesized from the acid-catalysed reaction of I,I'-diindolyl compounds and aryl aldehydes. Some reactions of these compounds and the attempted synthesis of 2,2' diindolylmethanes from the cyclic compounds have also been described. The electrophilic substitution reactions of 3-substituted 4,6-dimethoxyindole 2,6-dimethanols and 3-substituted 4,6-dimethoxyindole-7 and 2-carbaldehydes and I-substituted indoles afforded triindolyl dialdehydes. The wriation of substituents at C-7 of indole-7-aldehydes and at C-2 of indole-2-aldehydes has also been discussed. Reaction of the hydroxymethylindole and 1,2-di(indol-I-ylmethyl)benzene gave a new macrocycle. Substitution reactions of 2,2???-diindolylmethane-7,7'-dimethanol and indole-7- and 2-aldehydes gave tetraindolyl dialdehydes. Sodium borohydride reduction of tri- and tetra-indolyl dialdehydes gave tri- and tetra-indolyl dimethanols respectively. Acid-catalysed reactions of tri- and tetra-indolyl dimethanols afforded only calix[3] and [4]indoles respectively when all substituents at C-3 of indoles were aryl groups. New conditions for indole based imine synthesis have been established Macrocyclic imine formation from mono-, di-, tri and tetra-indolyl dialdehydes has been investigated. Reactions of indole-3, 7-dialdehydes and short chain diamines (1,2-diaminoethane, 1,2-diaminobenzene and 1,6-diaminohexane) gave mixtures while the reactions with long chain diamines (1,10 diaminodecane and 1,12-diaminododecane) gave monoindolyl macrocyclic imines. Reaction of indole-2, 7-dialdehydes and short chain diamines afforded diindolyl macrocyclic imines with head-tail structures, and the 2,7';2',2";7",2'''-Tetraindole-7 ,7"'-dialdehyde underwent cyclisation with triindolyl dialdehydes and 1,6-diaminohexane afforded triindolyl macrocyclic imines. 1,2 diaminoethane while the 2,3 ';1',1 ";3 ",2"'-tetraindole-7,7"'-dialdehydes underwent imine, with its precise structure established by X-ray crystallography. Reaction of of 1,3-di(indol-l-ylmethyl)benzene and 1,2 diaminoethane yielded a new macrocyclic reactions with long chain diamines yielded monoindolyl macrocyclic imines. Reaction ring closure with 1,2 diaminoethane and 1,6-diaminohexane.
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Banini, Serge R. "Palladium-catalyzed syntheses of indoles, pyrroloindoles, quinolines a base-mediated formation of N-alkoxyindoles, and progress toward the first total synthesis of echinosulfone A /." Morgantown, W. Va. : [West Virginia University Libraries], 2008. https://eidr.wvu.edu/etd/documentdata.eTD?documentid=5710.
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Thesis (Ph. D.)--West Virginia University, 2008.Title from document title page. Document formatted into pages; contains xv, 275 p. : ill. Includes abstract. Includes bibliographical references (p. 107-113).
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Gu, Ji-Dong. "Biodegradation of pesticide and indolic compounds under methanogenic conditions." Diss., Virginia Tech, 1991. http://hdl.handle.net/10919/39831.
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Degradability of atrazine, cyanazine, and dicamba under methanogenic conditions was evaluated using serum bottle microcosms containing wetland soil inocula obtained from three different sites. Pesticides were monitored by high-performance liquid chromatography (HPLC) and the production of methane was measured with a gas chromatograph (GC). Dicamba was the most susceptible to degradation in the microcosms, followed by cyanazine. Atrazine was not degraded in the wetland soils. A dicamba-degrading methanogenic consortium was enriched from one of the initial wetland soil microcosms (Lawnes). Dicamba degradation was further examined using this consortium. Net methane production suggested that the aromatic ring was not degraded. Rates of dicamba degradation were enhanced with addition of 0.2 % yeast extract.
Dicamba degradation was accomplished within 4 days compared to 22 days without yeast extract addition. The inability of the consortium to degrade the benzenoid ring was confirmed when no ¹⁴CO₂ was produced upon addition of [U-¹⁴C]dicamba to the cultures. Analysis of culture filtrate by HPLC revealed the presence of a possible metabolite that was aromatic in character.Ph. D.
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Pchalek, Karin Chemistry Faculty of Science UNSW. "Design and synthesis of new ligands and heterocycles from activated indoles." Awarded by:University of New South Wales. School of Chemistry, 2004. http://handle.unsw.edu.au/1959.4/20584.
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For the purpose of incorporating indoles into organometallic complexes for catalysis, as well as in the generation of new heterocyclic systems, various reactions have been carried out at C2, C6 and C7 of the indole system. In order to achieve this, 3-substituted 4,6-dimethoxyindoles and 6-hydroxy- 4-methoxyindoles were necessary as starting materials. Consequently, a lithium-bromide-templated one-pot procedure for the synthesis of some 3-substituted 4,6-dimethoxyindoles and a selective demethylation procedure for 3-substituted 6-hydroxy-4-methoxyindoles were developed. Various kinds of novel methylene-bridged bi-, tri-, and tetradentate pyridyl-indole ligands were synthesised via Vilsmeier-Haack, Friedel-Crafts or electrophilic addition reactions on the indole heterocycle. However, their metal complexing properties were generally weak and variable. Nevertheless, some of the tridentate pyridylindole ligands showed strong anion binding to halides, whereas a remarkable ligand transformation occurred with a bidentate 2-pyridylindole ligand and zinc(II), giving a substituted indolo[2,3-c]pyrrolo-[3,2,1-ij]quinoline system. Two new types of tetradentate Schiff base ligands were prepared from 2-formyl-indoles and 7-formyl-6-hydroxyindoles, and diamines. These preformed ligands were reacted with first- and second-row transition metals to give neutral metal complexes. Novel heterocyclic systems such as 4H-pyrrolo[3,2,1-ij]quinolines, 3H-pyrrolo-[1,2-a]indoles, and 1H-furo[2,3-g]indoles were synthesised from 2-formyl-, 7-formyl-, and 6-hydroxyindoles, utilising mainly intra-molecular Wittig reactions, Claisen-Schmidt condensations or acid- and base-catalysed cyclisations. A common feature of the prepared 4H-pyrrolo[3,2,1-ij]quinolines and 3H-pyrrolo-[1,2-a]indoles was their intense fluorescent character, which was examined as well.
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Souchet, Michel. "Synthese de la (+) anticapsine et d'analogues structuraux : evaluation de leurs proprietes biologiques." Paris 6, 1988. http://www.theses.fr/1988PA066545.
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Synthese du compose du titre et de ses derives perhydro indoliques via la synthese stereoselective d'alcools allyliques. Etude de l'activite inhibatrice des composes synthetises sur la glucosamine synthetase et sur l'enzyme de conversion de l'angiotensine
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Berkous, Rabiaa. "Greffage de modèles du NADH sur deux nouveaux supports insolubles. Synthèse et réactivité d'un modèle du NADH en série indolo (2,3-b)-pyridine : réduction de substrats non activés." Rouen, 1994. http://www.theses.fr/1994ROUES042.
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Le greffage de réactifs modèles du NADH a été réalisé sur deux nouveaux supports: un matériau mixte silice-polymère et un polymère acrylique à chiralité intrinsèque. Dans les deux cas, la réduction de substrats classiques a été possible. Avec le second support, une induction asymétrique a été observée. Afin d'effectuer la réduction de substrats non activés en présence d'acides de Lewis capables d'activer de tels substrats, un modèle en série indolo (2,3-)pyridinique a été synthétisé. Il est stable et possède une réactivité élevée. Il est le premier modèle du NADH à avoir permis la réduction quasi quantitative de l'acétophénone. Il a également permis de réduire une large gamme de cétones non activées. Le modèle chiral de la même série a réduit l'acétophénone et le phénylglyoxylate de méthyle avec des excès énantiomériques intéressants. Un modèle non chiral en présence d'acides de Lewis chiraux a aussi permis d'observer une induction asymétrique
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Koulibaly, Issa. "Automatisation et optimisation de la synthèse du ((pyridyl-4)-2 ethyl)-3 indole, précurseur d'un antidépresseur." Paris 6, 1986. http://www.theses.fr/1986PA066413.
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Dans le cadre des recherches concernant l'application des techniques d'automatisation et des méthodes d'optimisation, sur les procédés de fabrications industrielles de produits pharmaceutiques, nous avons choisi l'automatisation et l'optimisation de la synthèse d'un précurseur de l'indalpine, qui est un produit pharmaceutique important par ses propriétés d'antidépresseur. Nous montrons, dans la première partie de ce travail, qu'il est possible d'automatiser, à l'échelle du laboratoire, et pour un cout réduit, une synthèse organique complexe à l'aide d'un automate de bas de gamme et de capteurs et actionneurs adéquats, que l'automatisation nécessite une bonne description du mode opératoire; pour cela, nous avons utilisé le langage grafcet afin de structurer le mode opératoire industriel. Dans la deuxième partie, nous prouvons qu'il est aussi possible d'améliorer le rendement d'une synthèse organique en établissant la fonction réponse et en l'optimisant pour obtenir les coordonnées de l'optimum. Pour la synthèse concernée dans ce travail, le gain de rendement a été de 22 points.
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Kerbal, Abdelali. "Cycloaddition de diarylnitrilimines et d'azides sur diverses énones et énamines dérivées d'indadones et de tétralones : Regiochimie, diasteréochimie et transformation des cycloadduits." Besançon, 1988. http://www.theses.fr/1988BESA2038.
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La cycloaddition dipolaire-1,3 des diarylnitrilimines sur diverses enones a double-liaison dipolarophile juxtacyclique est regiospecifique. Lorsque le dipolarophile présente deux faces diastereotopiques, l'approche dipole-dipolarographie se fait du côté le moins encombré : - de façon diastereospecifique sur les enones dérivées de l'indanone-1 substituée ou de la tetralone-1 substituée lorsque ces dernières portent en -3 ou -4 un substituant occupant une position axiale - de facon diastereoselective sur les enones dérivées de la tetralone-1 portant un substituant en -4 qui peut adopter une disposition équatoriale. Ces résultats qui mettent en évidence l'importance des facteurs conformationnels, sont généraux et ont pu être étendus aux cas d'autres enones dérivées des chromanones et isothiochromanone
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Ferroud, Clotilde. "Étude de la réaction de Diels-Adler intra et intermoléculaire sous haute pression : application à la synthèse stéréosélective d'alcaloïdes de l'indole du groupe des yohimbanes." Paris 6, 1986. http://www.theses.fr/1986PA066023.
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Le schéma de synthèse repose sur une unité bicyclique, précurseur direct des unités (d,e) du squelette pentacyclique. Cet intermédiaire est basé sur une réaction de Diels-Alder sous haute pression, utilisant la cycloaddition de diènes de structure donneur-accepteur 1,4 avec une lactone insaturée comme diénophile. La synthèse du système pentacyclique est exposée à partir de cet intermédiaire clé.
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Grisoni, Serge. "Synthese biomimetique du cycle c des alcaloides de l'ergot : application, premiere synthese enantioselective de la (-) chanoclavine i." Paris 6, 1987. http://www.theses.fr/1987PA066408.
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Synthese de benzo (cd) indoles a partir de l'indolecarbaldehyde-4 par cyclisation intramoleculaire en presence de pd(o); l'utilisation de bases solides (alumine-kf ou k::(2)co::(3)) permet des conditions operationnelles douces
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Haelters, Jean-Pierre. "Synthèse de dérivés phosphono-indoliques-benzofuranniques et -pyrroliques à partir d'hydrazones phosphonates." Brest, 1987. http://www.theses.fr/1987BRES2002.
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Des derives phosphonoindoliques sont prepares par cyclisation d'arylhydrazones d'oxoalkylphosphonates selon fisher et par cyclodeshydratation d'arylamino-1 et arylamino-3 oxo-2 propylphosphonates selon bischler. Des indolyl-2 et indolyl-3 phosphonates, des indolylmethyl-2 et des indolylmethyl-3 phosphonates diversement substitues et leurs acides phosphoniques correspondants sont decrits. Toutes structures sont analysees par rmn **(1)h, **(31)p et 1**(3)c. L'analogue phosphore de l'intermediaire a aussi ete prepare. L'extention de la reaction de bischler aux aryloxycetones permet d'atteindre des benzofuryl-2 phosphonate et de benzofurylmethyl-3 phosphonates. Deux nouveaux reactifs sont utilises pour acceder aux arylaminocetones et aux aryloxycetones : les chloro-1 et chloro-3 methoxycarbonylhydrazono-2 propyl-phosphonates de diethyle, composes qui, traites en milieu basique, donnent des azoenes qui additionnent les anilines et les phenols. Ces azoenes additionnent aussi les carbanions, notamment les carbanions derives de cetones pour conduire, apres hydrolyse soit a des derives du pyrrole, soit a des dioxy-2, -5-alkylphosphonates precurseurs de cyclopentenones selon wittig-horner
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Debleds, François. "Complexation d'électrophiles aromatiques par des bases hétérocycliques ambidentes : structure et réactivité d'adduits carbones et azotes pyrroliques indoliques et imidazoliques." Paris 6, 1987. http://www.theses.fr/1987PA066330.
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Structure et formation des complexes de Meisenheimer du trinitro-1,3,5 benzène avec divers indoles, pyrroles, imidazoles ; étude cinétique de la décomposition de ces complexes. Etude cinétique de la protonation du kryptopyrrole en solution aqueuse.
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Alamgir, Mahiuddin Chemistry Faculty of Science UNSW. "Synthesis and reactivity of some activated heterocyclic compounds." 2007. http://handle.unsw.edu.au/1959.4/40831.
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An alternate approach to the synthesis of calix[3]indoles has been demonstrated, but further attempted synthetic approaches to calixindoles using new leaving groups led to uncharacterized polymeric products. The synthesis of new 7,7'-diindolylmethane- 2,2'-dicarbaldehydes gives potential for further ligand design and metal complex formation. In addition, 4,6-dimethoxyindole-7- carbaldehydes have been effectively converted to a range of 6-methoxyindole-4,7-diones by Dakin oxidation. Various electrophilic substitution reactions have been performed on the 4,6-dimethoxybenzimidazoles. Formylation, acylation, acid catalyzed addition of formaldehyde and nitration revealed that the activated benzimidazoles are less reactive at the specified C-7 position compared to the analogous indoles. The key starting material for a potential calixbenzimidazole was synthesized by the selenium dioxide oxidation of 2-methyl-7-formyl-4,6-dimethoxybenzimidazole and by oxidative cleavage of 4,6-dimethoxy- 2-styrylbenzimidazole by Lemieux-Johnson reagent followed by reduction. Nevertheless, attempted preparation of calixbenzimidazole from 2-hydroxymethyl-4,6-dimethoxy benzimidazole led to formation of a dibenzimidazolyl ether. The synthesis of some novel activated bisbenzimidazoles has been developed. Furthermore, benzimidazoles were incorporated into new ligand systems which have led to a wide range of acyclic quadridentate neutral metal complexes. Activated benzimidazoles overall illustrate one electron irreversible oxidation to form a radical cation followed by multielectron oxidations. On the other hand, the nickelII and cobaltII benzimidazole metal complexes investigated showed one electron ligand centered reversible reduction. Irreversible radical cation oxidation followed by multielectron oxidation of the metal complexes further demonstrates the rich electrochemical nature of the 4,6-dimethoxybenzimidazoles. Some novel 7-(indol-2-yl)-4,6-dimethoxybenzimidazoles were prepared with indolin-2-one and triflic anhydride and an alternate procedure afforded 2-(4,6-dimethoxyindol-7-yl)-benzimidazoles from activated indoles and 2-benzimidazolinone. Two new isomeric series of 2-substituted-5,7-dimethoxybenzothiazoles and 2-substituted-4,6-dimethoxybenzothiazoles were synthesized via Jacobson cyclization. The two strategically placed electron donating methoxy groups activate these benzothiazoles to undergo various electrophilic substitutions at the 4- and 7- positions respectively.
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Groom, Katherine. "Studies into the Biosynthesis and Chemical Synthesis of Indolocarbazoles and Related Heterocyclic Compounds. Metalation of Indole-6-Carboxamide." Thesis, 2013. http://hdl.handle.net/1974/7816.
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The electron rich and aromatic character of the indole group allows for a wide range of oxidative and substitution reactions, creating a versatile platform for generating structurally diverse molecules. This thesis explores enzyme and synthetic chemistries that act upon indoles and related molecules. Chapter 1 describes the results of in vivo studies of RebC, an enzyme that plays a pivotal role in the biosynthesis of the indolocarbazole alkaloid rebeccamycin. A homologous enzyme, StaC, exists in the biosynthetic pathway for staurosporine, a related indolocarbazole. Structural differences between the RebC and StaC active sites were hypothesized to play a pivotal role in determining the oxidation state in the corresponding natural products. Sequence alignment of RebC and StaC with homologous enzymes from related indolocarbazole biosynthetic pathways revealed six non-conserved residues in the active site. Three RebC variants were generated by replacement of all six, four, or two specific residues with their StaC counterparts. It was demonstrated that only two substitutions, F216V and R239N, are required to convert the specificity of RebC to that of StaC. Analysis of the structure of the RebC bound to a putative reaction intermediate supports the importance of F216 and R239 in catalysis. Based on these results, contrasting mechanisms for RebC and StaC are proposed to account for their differing specificities.
Chapter 2 describes a synthetic approach to primarily heterocyclic analogues of lycogarubin C. Suzuki coupling of appropriately functionalized 3,4-dibromopyrrole or 3,4-bis(trifluoromethanesulfonyl)pyrrole was effective for numerous π-excessive five-membered heterocyclic-3-boronic acids. The optimized conditions were less effective for cross-couplings involving heteroaromatic-2-boronic acids, π-deficient heteroaromatic boronic acids, and heteroaromatic boropinacolate esters. Oxidative cyclization of the 3,4-bis(thiophen-3-yl)pyrrole and 3,4-bis(benzothiophen-3-yl)pyrrole to give analogues of the corresponding indolocarbazoles was demonstrated.
Chapter 3 describes preliminary results on the development of regioselective C-5 and C-7 indole metalation tactics of indole-6-carboxamides, in order to provide new functionalized indoles. The use of an indole C-2 silicon protection strategy in combination with a sterically bulky C-6 N,N-di-isopropyl carboxamide directed metalation group overcame undesired side reactions observed with the analogous N,N-diethyl indole-6-carboxamide, affording the C-5 and C-7 substituted products in 40% and 13% yields, respectively.Thesis (Ph.D, Chemistry) -- Queen's University, 2013-02-13 11:14:49.599
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Li, Yang. "Tandem intramolecular photocycloaddition-retro-Mannich fragmentation as a route to indole and oxindole." Thesis, 2012. http://hdl.handle.net/1957/28312.
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Irradiation of a tryptamine linked through its side-chain nitrogen to an alkylidene malonate residue results in an intramolecular [2 + 2] cycloaddition to the indole 2,3-double bond. The resultant cyclobutane undergoes spontaneous retro-Mannich fission to produce a spiro[indoline-3,3-pyrrolenine] with relative configuration defined by the orientation of substituents in the transient cyclobutane. The novel tandem intramolecular photocycloaddition- retro-Mannich (TIPCARM) sequence leads to a spiropyrrolidine which is poised to undergo a second retro-Mannich fragmentation [TIPCA(RM)₂] that expels the malonate unit present in the photo substrate and generates transiently an indolenine. The indolenine undergoes rearrangement to a β-carboline which can undergo further rearrangement under oxidizing conditions to an oxindole. Three oxindole natural products, coerulescine, horsfiline and elacomine, were synthesized using this strategy.
The TIPCARM strategy was extended to an approach that would encompass the Vinca alkaloids vindorosine and minovine. In this case, the TIPCARM sequence was followed by an intramolecular cyclization that provided tetracyclic ketone 5.86 containing rings A, B, C and D of vindorosine. A tetracyclic intermediate was synthesized which could also provided access to the Vinca alkaloid minovine.Graduation date: 2012
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Lin, Lyu, and 林綠. "Efficient and Cost-free Protocols for the Synthesis of Heterocyclic Compound with Indole." Thesis, 2014. http://ndltd.ncl.edu.tw/handle/91424501317704535409.
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碩士國立臺灣師範大學
化學系
102
The thesis is divided into two chapters. The first chapter is subdivided into two sections. The first section chapter I describes the synthesis of pyrazole derivatives from the dibenzolideneacetone derivatives and phenylhydrazines via copper (I) iodide catalyzed one-pot oxidative C-H amination and aromatization. The pyrazole moiety is present in many important agrochemical and pharmaceutical products, such as the pesticides Cyenopyrafen, Tebufenpyrad, Tolfenpyrad, Fenpyroximate, and nonsteroidalanti-inflammatory drug Celecoxib. The second section of Chapter I deals with the synthesis of 1,3,4-oxadiazole derivatives. This method involves the reaction of indole adduct of dibenzolideneacetone derivatives with acylphenylhydrazine in the presence of acetic anhydride under microwave irradiation. This reaction did not need any metal or acidic catalyst. 1,3,4-oxadiazole derivatives possess biological activities and are common drugs structure. The chapter II describes the synthesis of carbazole derivatives from the reaction of indole adduct of dibenzolideneacetone phenylhydrazine and benzoquinone in absence of catalyst in toluene and acetic acid. A wide variety of substituted carbazole derivatives were synthesized in this procedure. Carbazole derivatives possess biological activities, such as Clausamines A-G shows activity of antitumor on Raji cell.
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Travica, S., Klaus Pors, Paul M. Loadman, Steven D. Shnyder, I. Johansson, Mohammed N. Alandas, Helen M. Sheldrake, S. Mkrtchian, Laurence H. Patterson, and M. Ingelman-Sundberg. "Colon cancer-specific cytochrome P450 2W1 converts duocarmycin analogues into potent tumor cytotoxins." 2013. http://hdl.handle.net/10454/6217.
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PURPOSE: Cytochrome P450 2W1 (CYP2W1) is a monooxygenase detected in 30% of colon cancers, whereas its expression in nontransformed adult tissues is absent, rendering it a tumor-specific drug target for development of novel colon cancer chemotherapy. Previously, we have identified duocarmycin synthetic derivatives as CYP2W1 substrates. In this study, we investigated whether two of these compounds, ICT2705 and ICT2706, could be activated by CYP2W1 into potent antitumor agents. EXPERIMENTAL DESIGN: The cytotoxic activity of ICT2705 and ICT2706 in vitro was tested in colon cancer cell lines expressing CYP2W1, and in vivo studies with ICT2706 were conducted on severe combined immunodeficient mice bearing CYP2W1-positive colon cancer xenografts. RESULTS: Cells expressing CYP2W1 suffer rapid loss of viability following treatment with ICT2705 and ICT2706, whereas the CYP2W1-positive human colon cancer xenografts display arrested growth in the mice treated with ICT2706. The specific cytotoxic metabolite generated by CYP2W1 metabolism of ICT2706 was identified in vitro. The cytotoxic events were accompanied by an accumulation of phosphorylated H2A.X histone, indicating DNA damage as a mechanism for cancer cell toxicity. This cytotoxic effect is most likely propagated by a bystander killing mechanism shown in colon cancer cells. Pharmacokinetic analysis of ICT2706 in mice identified higher concentration of the compound in tumor than in plasma, indicating preferential accumulation of drug in the target tissue. CONCLUSION: Our findings suggest a novel approach for treatment of colon cancer that uses a locoregional activation of systemically inactive prodrug by the tumor-specific activator enzyme CYP2W1.