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Dissertations / Theses on the topic 'Piperidine derivatives'

Author: Grafiati

Published: 4 June 2021

Last updated: 25 April 2022

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1

Girling, Paul Ricardo. "Novel approaches to piperidine and hydropyridine derivatives." Thesis, Durham University, 2012. http://etheses.dur.ac.uk/6354/.

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Three new modes of reactivity are reported between the reaction of an imine, but-3-en-2-ones and a Lewis acid. These are formal [2+2+2]-, [1+2+1+2]- and [4+2]- cycloadditions, deriving 1,1'-(1,2-dihydropyridine-3,5-diyl)diethanones, 1,1'-(1,4-dihydropyridine-3,5-diyl)diethanones and piperidin-4-ones and respectively. The [2+2+2]- and [1+2+1+2]-cycloadditions proceed when R3 = LG (leaving group), with the [1+2+1+2]-pathway dominating when the imine is easily hydrolysed within the reaction conditions. When R3 ≠ LG, the cycloaddition proceeds through different [4+2]-mechanistic pathways, dependen

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2

Woods, Gordon Alexander. "Synthetic approaches to functionalised piperidines." Thesis, University of Oxford, 1999. http://ora.ox.ac.uk/objects/uuid:4c6fdb6c-c021-447c-8fc9-35241b552850.

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This thesis is concerned with the synthesis of functionalised piperidines. The piperidine unit is found in numerous alkaloids and other natural products, and has also been incorporated into synthetic compounds of significant therapeutic or strategic synthetic potential. Although numerous syntheses of individual piperidine compounds have been published, there are few general routes to this class of compounds, and there is therefore a need for such routes to be developed. Bicyclic lactams derived from (S)-pyroglutamic acid have been shown to be useful synthons in the synthesis of pyrrolidines. A

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3

Smith, Peter Duncan. "Synthesis of pipecolic acid derivatives via aza-Diels-Alder reactions." Thesis, Heriot-Watt University, 2000. http://hdl.handle.net/10399/552.

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4

Moraux, Thomas. "Synthesis and evaluation of α-fluoro analogues of capsaicin and 2-(aminomethyl)piperidine derivatives". Thesis, University of St Andrews, 2011. http://hdl.handle.net/10023/2094.

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Chapter 1 gives an overview of the fluorine chemistry field, from its early developments to recent applications in medicinal chemistry. The development of asymmetric electrophilic or nucleophilic installation of fluorine in organic molecules is highlighten. Chapter 2 of this thesis discusses the enantioselective synthesis of α-fluoroamides. The study is applied to the synthesis of fluoroenantiomers of the bioactive molecule capsaicin and short-chain analogues. The biological activity of these compounds is assayed with the TRPV1 receptor. Results show that enantioselective α-fluoroamides (R)-97

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5

Petrov, Ravil Rashitovich. "Part I. Application of 2-Hydroxymethylacrylic Acid, a Product of Baylis-Hillman Reaction, for the Synthesis of Novel N-backbone-to-Side-Chain Cyclic Peptide Analogs: Strategies and Side Reactions Part II. Synthesis and Biological Activities of Chimeric Bioactive Peptides Featuring Amino Acids Coupled to 4-Anilino-N-Phenethyl-Piperidine." Diss., The University of Arizona, 2007. http://hdl.handle.net/10150/194330.

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During my research career in Prof. V.J.Hruby's laboratory I worked on two different projects. The first project, which was initiated by the author, was planned to serve the need of our laboratory for a novel method of peptide cyclization. This method was planned to use recent advances in Pd0-catalyzed asymmetric synthesis combined with the structural richness offered by the Baylis-Hillman chemistry which could open new ways to diverse areas of drug design, molecular immunology and chemotherapy. This approach would provide cyclic peptides featuring N-alkylated amino acids that would confer high

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6

Anhettigama, Gamaralalage Medha Jaimini Gunaratna. "Design, synthesis and bio-evaluation of piperidines and CGRP peptides; Synthesis of substituted 6-(dimethylamino)-2-phenylisoindolin-1-ones for the inhibition of luciferase." Diss., Kansas State University, 2017. http://hdl.handle.net/2097/38204.

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Doctor of Philosophy<br>Department of Chemistry<br>Duy H. Hua<br>Three research projects are described in this dissertation, and they are: (i) discovery of piperidine derivatives as T-type calcium channel inhibitors for the treatment of epilepsy and neuropathic pain and as protein disulfide isomerase inhibitors for the treatment of influenza viral infection; (ii) discovery of peptide-based calcitonin gene-related peptide receptor antagonists for the treatment of inflammatory pain; and (iii) synthesis of substituted 6-(dimethylamino)-2-phenylisoindolin-1-ones for the inhibition of luciferase.

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7

Hunter, Darren F. A. "Synthesis of bioactive pyrrolidine and piperidinone derivatives from carbohydrates." Thesis, University of Oxford, 2001. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.418528.

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8

Wong, Yung-Sing. "Nouveaux intermediaires chiraux de type 1,4-dihydropyridine et equivalents de sels de 3,4-dihydropyridinium pour la synthese asymetrique de piperidines polysubstituees. Application a la synthese enantioselective du 3-ppp et de l'indolizidine 195b." Paris 11, 1994. http://www.theses.fr/1994PA112105.

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L'application de la reaction de zincke a des amines primaires enantiomeriquement pures a donne des sels de pyridinium portant un centre asymetrique directement fixe sur l'azote, a partir de la pyridine correspondante, substituee ou non en position 3. L'etude de la reduction par le dithionite de sodium de ces sels a conduit de maniere efficace a de nouveaux intermediaires 1,4-dihydropyridines chiraux. La reduction des sels n-substitues par une chaine phenylethanol donne des 1,4-dihydropyridines qui s'isomerisent en 3,7,8,8a-tetrahydro-2h-oxazolo3,2-apyridines. Une etude structurale a ete entrep

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9

Othman, Arige. "Pharmacomodulation on the piperidinol skeleton: Synthesis of novel PIPD1 derivatives as Mycobacterium abscessus agents." Master's thesis, Alma Mater Studiorum - Università di Bologna, 2017. http://amslaurea.unibo.it/13396/.

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Mycobacterium abscessus (M. abscessus) is a rapidly growing mycobacterium which is able to generate different problems in human infections, such as chronic lung diseases, pulmonary diseases and skin infection. M. abscessus is considered as the first emergent opportunistic pathogen and the number of the infections due to this pathogen increases each year. Since the natural multidrug resistance and the absence of specific treatment to fight it, M. abscessus has become a serious problem of the public health. In this context, an original approach of a phenotypic screen was performed and allowed to

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10

Thaler, Tobias. "Enantiocontrol with Chiral Sulfoxides and Diastereocontrol in the Cross-Couplings of Substituted Cycloalkyl and Piperidinyl Derivatives." Diss., lmu, 2011. http://nbn-resolving.de/urn:nbn:de:bvb:19-134189.

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11

Thaler, Tobias Johannes Werner [Verfasser], and Paul [Akademischer Betreuer] Knochel. "Enantiocontrol with Chiral Sulfoxides and Diastereocontrol in the Cross-Couplings of Substituted Cycloalkyl and Piperidinyl Derivatives / Tobias Thaler. Betreuer: Paul Knochel." München : Universitätsbibliothek der Ludwig-Maximilians-Universität, 2011. http://d-nb.info/1015170943/34.

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12

Naicker, Leeantha. "Pharmacological screening of synthetic piperidine derivatives." Thesis, 2016. http://hdl.handle.net/10321/1734.

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Submitted in complete fulfillment for the Degree of Master of Applied Sciences in Biotechnology, Durban University of Technology, Durban, South Africa, 2016.<br>Piperidine derivatives are essential heterocyclic compounds that have beneficial roles in the medical and commercial sector. They can be isolated from plant material and can be chemically synthesised using simple cost efficient methods. Piperidines and their derivatives are clinically used to prevent postoperative vomiting, facilitate radiological evaluation, correct gastrointestinal function as well as speed up gastric emptying before

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13

Shey, Jing-Ying, and 徐錦英. "Soluble Polymer-Supported Combinatorial Synthesis Piperidine and Piperazine Derivatives." Thesis, 1999. http://ndltd.ncl.edu.tw/handle/20405295067465780839.

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碩士<br>國立東華大學<br>化學研究所<br>87<br>Abstract Combinatorial synthesis of chemistry libraries is undergoing rapid examination as a tool to enhance drug research and development. While it appears obvious that combinatorial chemistry strategies offer the potential to enhance drug development by shortening the time to optimize a new lead by structure-activity relationship (SAR) studies, it is often less appreciated that the greatest value of combinatorial chemistry strategies lies in its potential to enhance discovery of novel leads or pharma- cophores. The development of both

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14

Chen, Guei-Tang, and 陳貴棠. "Studies on Syntheses of Enantiomeric Pure 2,6-piperidine and 7-azanorborane Derivatives." Thesis, 2011. http://ndltd.ncl.edu.tw/handle/39268846969005440976.

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碩士<br>國立中興大學<br>化學系所<br>99<br>Studies on syntheses of enantiomeric pure 2,6-piperidine derivatives by chiral resolution of aminoalcohol. Syntheses of enantiomeric pure 7-azanorborane derivatives by using chiral auxiliary.

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15

Afarinkia, Kamyar, A. Bahar, M. J. Bearpark, et al. "An Investigation of the Diels-Alder Cycloadditions of 2(H)-1,4-Oxazin-2-ones." 2005. http://hdl.handle.net/10454/3750.

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No<br>Forumla chem. . A variety of 5-chloro-2(H)-1,4-oxazin-2-ones bearing a range of substituents at their 3- and 6-positions undergo Diels-Alder cycloaddition as a 2-azadiene component with electron-rich, electron-deficient, and electron-neutral dienophiles. These reactions proceed with moderate regio- and stereoselectivity to afford relatively stable and readily isolable bridged bicyclic lactone cycloadducts. Chemical manipulation of these cycloadducts affords highly substituted and functionally rich piperidines. The regio- and stereochemical preferences of the cycloadditions of 5-chloro-2(

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16

St-Onge, Miguel. "Synthèse stéréosélective de dérivés pipéridines polysubstitués par fragmentation de Grob." Thèse, 2008. http://hdl.handle.net/1866/3472.

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Dans ce mémoire, il sera question de la formation de dérivés pipéridines en utilisant la fragmentation de Grob. Tout d’abord, une introduction sur les alcaloïdes ainsi que sur l’expertise du groupe Charette associée à leur formation démontrera l’importance de ces composés dans le domaine de la chimie organique. Cela sera suivi par un résumé de la fragmentation de Grob incluant les conditions de réactions utilisées, l’importance de la structure de la molécule initiale, les prérequis stéréoélectroniques ainsi que les modifications qui y ont été apportées. Le chapitre 2 sera dédié au développem

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17

Kuo, Wei-Shen, and 郭威伸. "Synthesis of a New Trihydroxy Piperidine Derivative for Glycosidase Inhibitor from D-(-)-Quinic Acid." Thesis, 2004. http://ndltd.ncl.edu.tw/handle/86579139954835053864.

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碩士<br>淡江大學<br>化學學系<br>92<br>Recently, the syntheses of glycosidase inhibitors have attracted a great deal of attention in academies and industries. These glycosidase inhibitors possess potential in the treatment of cancers, HIV, diabetes and metabolic disorders.The polyhydroxylated piperidines (called “azasugars” or “iminosugars”) have been known as glycosidase inhibitors. They display the same stereochemical information as common hexoses, but a nitrogen atom replaced the ring oxygen of the corresponding pyranose. Among these azasugars, the representative morecu1es, such as 1-deoxynojirimycin

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18

Teesdale-Spittle, P. H., Klaus Pors, R. Brown, Laurence H. Patterson, and J. A. Plumb. "Development of nonsymmetrical 1,4-disubstituted anthraquinones that are potently active against cisplatin-resistant ovarian cancer cells." 2005. http://hdl.handle.net/10454/3191.

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No<br>A novel series of 1,4-disubstituted aminoanthraquinones were prepared by ipso-displacement of 1,4-difluoro-5,8-dihydroxyanthraquinones by hydroxylated piperidinyl- or pyrrolidinylalkyl-amino side chains. One aminoanthraquinone (13) was further derivatized to a chloropropyl-amino analogue by treatment with triphenylphosphine-carbon tetrachloride. The compounds were evaluated in the A2780 ovarian cancer cell line and its cisplatin-resistant variants (A2780/ cp70 and A2780/MCP1). The novel anthraquinones were shown to possess up to 5-fold increased potency against the cisplatin-resistant ce

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19

Chen, I.-Hsiang, and 陳宜香. "Design and Synthesis of 1-(6-(2-(2-(2-Aryl)ethynyl)phenyl)hex-5-ynyl)piperidin-2-ones Derivatives to induce Apoptotic Progress with Antitumor Activity." Thesis, 2007. http://ndltd.ncl.edu.tw/handle/95636210811543295377.

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碩士<br>高雄醫學大學<br>醫藥暨應用化學研究所碩士班<br>95<br>1-(6-(2-(2-(2-Aryl)ethynyl)phenyl)hex-5-ynyl)piperidin-2-ones 46-57 were designed and synthesized to evaluate for cell cycle of human leukemia K-562 tumor cell line, and the cytotoxic responses against sixty human tumor cell line. Some of compounds presented biological activities in this evaluation course, in which compounds 47 and 48 exhibited S phase arrested activities and compounds 55 and 56 induced apoptotic progress。

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