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Dissertations / Theses on the topic 'Quinazoline synthesis'

Author: Grafiati

Published: 4 June 2021

Last updated: 5 February 2022

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1

Larraufie, Marie-Hélène. "Development of new radical cascades and multi-component reactions : application to the synthesis of nitrogen-containing heterocycles." Paris 6, 2011. http://www.theses.fr/2011PA066516.

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Le travail décrit dans ce manuscrit de thèse est consacré au développement de nouvelles méthodes radicalaires et organométalliques permettant la synthèse de différentes classes de polycycles azotés. Nous avons étudié des cascades impliquant le motif N-acylcyanamide. Des précurseurs de type alkyle ont permis la synthèse de quinazolinones naturelles. L’utilisation de précurseurs vinyliques a permis de mettre à jour un processus de migration original, qui apporte de nouveaux éléments pour la compréhension du mécanisme de substitution aromatique homolytique. Enfin des radicaux aminyles ont pu être

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2

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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3

Raux, Elizabeth A. "Synthesis of Selective 5-HT6 and 5-HT7 Receptor Antagonists." Digital Archive @ GSU, 2010. http://digitalarchive.gsu.edu/chemistry_theses/32.

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The development of novel selective 5-HT6 and 5-HT7 receptor antagonists is an ever-growing area of interest among medicinal chemists. The potential of developing a therapeutic agent useful as an antipsychotic or antidepressant, as well as the possibility to develop a drug for Alzheimer’s disease and obesity has led to an increase in synthesis of possible lead compounds. The synthesis of unfused biheteroaryl derivatives is described within. The derivatives have been evaluated for binding affinity at 5-HT2A, 5-HT6 and 5-HT7 receptors. The most potent 5-HT6 receptor antagonists include a benzene

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4

Belfrage, Anna Karin. "Design and Synthesis of Hepatitis C Virus NS3 Protease Inhibitors : Targeting Different Genotypes and Drug-Resistant Variants." Doctoral thesis, Uppsala universitet, Avdelningen för organisk farmaceutisk kemi, 2015. http://urn.kb.se/resolve?urn=urn:nbn:se:uu:diva-243317.

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Since the first approved hepatitis C virus (HCV) NS3 protease inhibitors in 2011, numerous direct acting antivirals (DAAs) have reached late stages of clinical trials. Today, several combination therapies, based on different DAAs, with or without the need of pegylated interferon-α injection, are available for chronic HCV infections. The chemical foundation of the approved and late-stage HCV NS3 protease inhibitors is markedly similar. This could partly explain the cross-resistance that have emerged under the pressure of NS3 protease inhibitors. The first-generation NS3 protease inhibitors were

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5

Doan, Thu Hong. "Synthesis, self-assembly and photophysical evaluation of fluorophores derived from acenes, heteroacenes and quinazolines." Thesis, Normandie, 2018. http://www.theses.fr/2018NORMC205.

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Les semiconducteurs organiques (OSC) tels que les composés organiques photovoltaïques (OPVs), les diodes électroluminescentes organiques (OLEDs) ou encore les transistors organiques à effet de champ (OFETs) constituent un domaine de recherche très attractif en raison de leur potentiel en tant que couches actives dans les dispositifs optoélectroniques. Les composés aromatiques polycycliques ainsi que les hétéroaromatiques sont considérés comme des matériaux prometteurs pour les OSC en raison de leurs conductivités électriques potentielles, de leurs propriétés optiques ainsi que de leurs assembl

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6

Hamed, Mostafa Mohamed Mostafa [Verfasser], та Rolf W. [Akademischer Betreuer] Hartmann. "Design and synthesis of novel quinazoline-based EGFR kinase inhibitors and dual EGFR/NF-κB inhibitors as potential anti-cancer drugs with enhanced efficacy / Mostafa Mohamed Mostafa Hamed. Betreuer: Rolf W. Hartmann". Saarbrücken : Saarländische Universitäts- und Landesbibliothek, 2013. http://d-nb.info/1078017077/34.

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7

Stein, Tobias. "Radical synthesis of quinazolinone natural products." Thesis, Loughborough University, 2007. https://dspace.lboro.ac.uk/2134/34389.

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Investigations into radical and palladium(0) cyclisations onto the C-2 position of the 3H-quinazolin-4-one moiety have been made. This has led to the syntheses of a number of biologically active quinazolinone natural products using alkyl, heteroaryl and acyl radical cyclisations. The reactions proceeded via a homolytic aromatic substitution mechanism. As such, fully rearomatised products were recovered. A C-2 radical 3H-quinazolin-4-one building block was also prepared. This turned out to have only limited synthetic applications. Radical cyclisations onto aryl groups were carried out using thi

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8

Norrie, R. "The synthesis and reactions of sulphur analogues of deoxyvasicinone." Thesis, University of Abertay Dundee, 1989. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.233850.

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9

Dai, Xuedong 1970. "Synthesis and applications of atropisomeric quinazolinone phosphine ligands." Thesis, Massachusetts Institute of Technology, 1998. http://hdl.handle.net/1721.1/47887.

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Thesis (Ph.D.)--Massachusetts Institute of Technology, Dept. of Chemistry, 1998.<br>Includes bibliographical references.<br>Several novel atropisomeric phosphine ligands have been synthesized and evaluated. The syntheses of 2-methyl-3-[2'-(diphenylphosphino)phenyl]-4(3H)- quinazolinone (la) and its methyl-substituted analogs lb and ic were achieved in good yield by coupling N-acetylanthranilic acid with the corresponding phosphinoanilines 4a-c. A practical resolution of ligands la-c was accomplished using the benzenesulfonylhydrazone derivative (10) of (1S)-(+)-camphorsulfonic acid as a novel

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10

Pertusati, Fabrizio. "Synthesis of atropisomeric 2,2'-disubstituted-3,3'-quinazolin-4,4'-diones and their application in asymmetric synthesis." Thesis, Cardiff University, 2007. http://orca.cf.ac.uk/54687/.

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This thesis reports all the efforts made in the synthesis of 2,2'-disubstituted-3,3'-quinazolin-4,4'-ones (BiQ), a new class of atropisomeric molecules derived from the 4-quinazolinone scaffold, and their potential application as chiral auxiliaries in asymmetric synthesis. Chapter 1 provides first an overview of axial chirality and atropisomerism and then it reports a review of asymmetric reactions such as Diels-Alder, 1,3-dipolar cycloaddition, epoxydation and cyclopropanation, which have been used in literature as a model for the development of new chiral auxiliaries and chiral ligands. Chap

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11

Owusu-Dapaah, George. "Synthesis and evalulation of new 1,4-benzodiazepinediones and quinazolines as antileishmanial agents." Thesis, University of Strathclyde, 2008. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.488755.

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12

Benjamin, Stefan Jason. "Synthesis and SAR investigation of haemozoin-inhibiting quinazolines active against Plasmodium falciparum." Master's thesis, University of Cape Town, 2016. http://hdl.handle.net/11427/22738.

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Malaria is a potentially fatal blood disease with most deaths caused by Plasmodium falciparum. It exists in 95 countries worldwide and puts nearly 3.2 billion people at risk of contracting the disease. Despite recent advances made in malaria eradication and control including by antimalarial drugs (the mainstay of malaria prophylaxis and disease treatment), the need for new antimalarials due to antimalarial drug resistance which is on the rise, means that malaria research remains an extremely important focus. In this study, 21 derivatives of a biologically relevant scaffold, 2,4-diaminoquinazol

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13

Harris, N. V. "Studies on the synthesis and antibacterial activities of 5- and 6-substituted quinazolines." Thesis, Open University, 1985. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.305151.

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14

Lindgren, Anders. "Synthesis of Small Molecules Targeting ADP-Ribosyltransferases and Total Synthesis of Resveratrol Based Natural Products." Doctoral thesis, Umeå universitet, Kemiska institutionen, 2015. http://urn.kb.se/resolve?urn=urn:nbn:se:umu:diva-108010.

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Diphtheria Toxin-like ADP-Ribosyltransferases The Human ADP-ribosyl transferases (ARTDs) are a group of poorly studied enzymes which are believed to be involved in e.g. DNA repair, protein degradation, transcription regulation and cell death. Medicinal chemistry programmes aimed at developing selective inhibitors of these ARTDs were initiated. A suitable starting compound for one of these enzymes, ARTD3, was found by screening a library of NAD-mimics using a thermal shift assay. A virtual screening protocol was instead developed in order to find novel inhibitors of ARTD7, 8, and 10. The hit co

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15

Malecki, Natacha. "Conception et synthese de derives quinoleiniques et quinazoliniques inhibiteurs potentiels des topoisomerases i et ii." Lille 2, 2001. http://www.theses.fr/2001LIL2P251.

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16

Quevedo, Camilo E. "Design and synthesis of Quinazolinone-based libraries for inhibitation of Kinase activity and hit-to-lead optimisation of Wnt pathway inhibitors." Thesis, Institute of Cancer Research (University Of London), 2008. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.510367.

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17

Huang, Ya-Ping, and 黃雅蘋. "Synthesis and Antiproliferative Evaluation of Substituted Quinazoline Derivatives." Thesis, 2012. http://ndltd.ncl.edu.tw/handle/29298330647027420014.

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碩士<br>高雄醫學大學<br>醫藥暨應用化學研究所<br>100<br>Quinazoline derivatives have been found to possess a wide variety of biological activities. The aims of this thesis are to synthesize and evaluate a series of 4-substituted and 2-substituted-vinyl quinazoline derivatives. These 4-substituted and 2-substituted-vinyl quinazoline derivatives with various substituents at the C-4 position of quinazoline skeleton and at the vinyl moiety have been synthesized and evaluated for their antiproliferatve activities. Results indicated that most of these newly synthesized compounds exhibited potent activities against the

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18

Chuang, Ming-Hsueh, and 莊明學. "Design and Synthesis of Quinazoline Derivatives as Potential Antitumor Agents." Thesis, 2016. http://ndltd.ncl.edu.tw/handle/73920432922782901061.

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博士<br>靜宜大學<br>應用化學系<br>104<br>In this thesis, a series of 2-, 4-, 6, and 7-substituted quinazoline derivatives were designed and synthesized as well as their cytotoxicities againststomach cancer cell line AGS, lung cancer cell lines A549, hepatocellular liver carcinoma cell line HepG2, colon cancer cell line HT-29 andprostate cancer cell line PC-3 were evaluated. Target compounds 4a,b and 6a,b are 4-cyclohexylamino/cyclohexanemethylamino and 2-(substituted anilino) substituted quinazoline. Among them, 4b and 6a possess moderate inhibitory activity against HT-29. Introducing methoxy groups onto

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19

Pao, Kuan-Chuan, and 鮑冠全. "Design and Synthesis of Novel Quinazoline Derivatives as CIP2A-Ablating Agents." Thesis, 2012. http://ndltd.ncl.edu.tw/handle/69444822770617253977.

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碩士<br>國立陽明大學<br>生物藥學研究所<br>100<br>Cancerous inhibitor of PP2A (CIP2A) is a novel oncoprotein which could stabilize the c-Myc by inhibiting PP2A (protein phosphatase 2 A) activity toward c-Myc and promoting anchorage-independent cell growth and in vivo tumor formation. Particularly, overexpression of CIP2A on several solid- and non-solid tumors has been recorded on document, including human neck and head carcinomas, colon, breast, cervical, prostate cancer, and acute leukemia. Recent studies have shown that small molecules, such as Velcade and Tarceva, exhibited the ability to downregulate the

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20

盧冠宇. "Synthesis and pharmacological evaluation of fused tricyclic thieno [2,3-d] pryimidine and quinazoline derivatives." Thesis, 1991. http://ndltd.ncl.edu.tw/handle/53126416670356751342.

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21

chou, Su-Lun, and 周書論. "Synthesis and Evaluation Anti-proliferation Ability of Quinazoline bearing Oxime, Methyloxime and Amide Derivatives." Thesis, 2014. http://ndltd.ncl.edu.tw/handle/43051299260201664769.

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碩士<br>大仁科技大學<br>製藥科技研究所<br>102<br>The quinazoline (QA) is a heterocyclic compound with benzene fused to pyrimidine and is a well-leading structure for new drug development because it displays a wide spectrum of pharmacological activities such as neuron protective, anti-bacterial and anti-cancer properties. In this study, we have synthesized a series of novel QA derivatives and evaluated their anti-proliferative mechanisms. Firstly, QA series were subjected to MTT assay to examine the growth-inhibitory abilities against three human cancer cell lines, including nasopharyngeal cancer (NPC-TW01),

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22

Brocklesby, K. L., Jennifer S. Waby, C. Cawthorne, and G. Smith. "An alternative synthesis of Vandetanib (CaprelsaTM) via a microwave accelerated Dimroth rearrangement." 2017. http://hdl.handle.net/10454/17298.

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Yes<br>Vandetanib is an orally available tyrosine kinase inhibitor used in the treatment of cancer. The current synthesis proceeds via an unstable 4-chloroquinazoline, using harsh reagents, in addition to requiring sequential protection and deprotection steps. In the present work, use of the Dimroth rearrangement in the key quinazoline forming step enabled the synthesis of Vandetanib in nine steps (compared to the previously reported 12–14).<br>This work was supported by the Cancer Research UK-Cancer Imaging Centre (grant: C1060/ A16464), the Institute of Cancer Research and the University

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23

Chiou, Maw-Shyang, and 邱茂祥. "Design and synthesis of oxime, methyloxime, amide containing quinazoline derivatives and evaluation anti-proliferative activity." Thesis, 2015. http://ndltd.ncl.edu.tw/handle/33514136455255431308.

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碩士<br>大仁科技大學<br>製藥科技研究所<br>103<br>The Quinazoline is a nitrogen-containing heterocyclic skeleton of benzene and pyrimidine being formed, many quinazoline compounds islated from porducts having broad pharmacological activity including neuronal protection, anti-bacterial and anti-tumor, and therefore subject to a considerable degree in drug development emphasis. In this study, we extend the results before continuing the synthesis of a series of oxime-containing, quinazolinone derivative of methyl oxime and amide and assess its antiproliferative activity in. The assessments were selected to seven

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24

Dilebo, Kabelo Bramley. "Synthesis and biological activity of schiff based and ruthenium P-Cymene complexes containing ethynylpyridine bridged to quinazoline derivatives." Thesis, 2019. http://hdl.handle.net/10386/3179.

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Thesis(M.Sc. (Chemistry)) -- University of Limpopo, 2019<br>Imidazolyl-ethanamine Schiff base ligands of the N^N type were prepared by condensation reaction of histamine dihydrochloride with para-substituted aldehyde derivatives to yield: (E)-N-benzylidene-2-(1H-imidazol-4-yl)ethanamine 119a, 4-((E)(2-(1H-imidazol-4-yl)ethylimino)methyl)phenol 119b, E)-N-(4-fluorobenzylidene)-2(1H-imidazol-4-yl)ethanamine 119c and (E)-N-(4-nitrobenzylidene)-2-(1H-imidazol-4yl)ethanamine 119d, which were characterised by 1H and 13C-NMR, FTIR specroscopy and HRMS. 2D-NMR experiments (1H-1H COSY and 2D-HMBC) for

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25

Chen, Mei-Yu, and 陳美玉. "Design and Synthesis of Quinazoline Derivatives as Potential Non-Peptide Corticotropin-Releasing Hormone Receptor (CRH1) Antagonists." Thesis, 2002. http://ndltd.ncl.edu.tw/handle/04213898628785511139.

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碩士<br>國立臺灣大學<br>藥學研究所<br>90<br>Abstract This thesis is aimed to design and synthesize substituted arylquinazoline derivatives as potential non-peptide corticotropin-releasing hormone 1 (CRH1) receptor antagonists. According to the structure-activity relationship of a series of known CRH1 antagonists and the lead compound CP154526-1 (12), quinazoline core was intended to replace the pyrrolopyrimidine ring leading to the target compounds 8-aryl-4-(N-cyclopropylmethyl-N-propylamino)- 2-methylquinazol-ines (36-38, 40). 2-Bromoaniline (20) was the starting material to prepare 2-bromoison

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26

Nowacka, Anna Elzbieta. "Divalent Metal Organic Frameworks as Heterogeneous Oxidation Catalysts." Doctoral thesis, 2019. http://hdl.handle.net/10251/129872.

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[ES] Se ha desarrollado un método de síntesis "verde" de compuestos metal orgánicos en medio acuoso, a temperatura y presión ambientes, fácilmente escalable y con tiempos de cristalización muy cortos (10 min). El método se ha aplicado con éxito a la síntesis de trimesatos de metales divalentes isoreticulares y con fórmula general M3(BTC)2·12 H2O (M = Ni2+, Co2+, Cu2+ y Zn2+; BTC = trimesato). La estructura de estos materiales presenta dos tipos de centros metálicos ("puente" y "ter-minales") en proporción 2 a 1, ambos con coordinación octaédrica y unidos a 4 moléculas de H2O y a dos oxígenos c

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27

Maluleka, Marole Maria. "Synthesis, biological evaluation and molecular docking studies of novel indole- and benzofuran-chalcone and benzofuran-quinazoline hybrids as anticancer agents." Thesis, 2019. http://hdl.handle.net/10500/25821.

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Text in English<br>Specially prepared 2-amino-5-bromo-3-iodoacetophenone and 5-bromo-2-hydroxy-3 iodoacetophenone were subjected to Claisen-Schmidt aldol condensation with benzaldehyde derivatives followed by sequential and/or one-pot palladium catalyzed Sonogashira cross coupling and heteroannulation of the 3-alkynylated intermediates to afford indole-chalcones and benzofuran-chalcones, respectively. The indole-chalcones derivatives were, in turn, subjected to trifluoroacetic anhydride in tetrahydrofuran under reflux to afford the corresponding 3-trifluoroacetyl substituted indole-chalcone d

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28

Chuang, Wei-Chung, and 莊維仲. "Lewis acid-mediated rearrangement of 4-imino-4H-3,1-benzoxazins : total synthesis of pyrazino[2,1-b]quinazoline-3,6-diones on solid support." Thesis, 2007. http://ndltd.ncl.edu.tw/handle/04011786751263321864.

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碩士<br>國立中正大學<br>化學所<br>96<br>Abstract Alkaloid pyrazino[2,1-b]quinazoline-3,6-diones contain structural motifs of quinazolinone and diketopiperazine-like skeletons. Some of which were found to have bioactivities. The last two steps in the organic synthesis of alkaloid pyrazino[2,1-b]quinazoline-3,6-diones involve the synthesis of peptides, which then undergo a cyclization-upon-deprotection reaction to form the final product. To perform peptide synthesis and cyclization-upon-deprotection, our and other laboratories have traditionally used liquid phase peptide synthesis and a combination of tr

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29

Ling, Mei, and 傅美玲. "The Syntheses of Quinazoline Intermediate of ?Blocker." Thesis, 2005. http://ndltd.ncl.edu.tw/handle/72691939932174536183.

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碩士<br>國立中正大學<br>化學工程所<br>93<br>2-Amino-4-chloro-6,7-dimethoxyquinazoline is a common key intermediate of some a-blocker anti-hypertension drugs including Prazosin, Doxazosin, and Terazosin. The preparation of 2-amino-4-chloro-6,7-dimethoxyquinazoline was first reported by Pfizer pharmaceutical company. Some modifications have been done in order to achieve economic scale-up and mass production towards those anti-hypertension drugs.

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30

Nan-Yi, Lai, and 賴南禕. "Synthesis and Pharmacological Evaluation of Quinaznolinones and Quinazolinone Analogs." Thesis, 1994. http://ndltd.ncl.edu.tw/handle/19598062278458444292.

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31

Chen, Hui-ting, and 陳惠亭. "Design and Synthesis of Indolo[2,1-b]quinazolin-6,12-dione Derivatives as Potential Antitumor Agents." Thesis, 2000. http://ndltd.ncl.edu.tw/handle/08556359314799771207.

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博士<br>國立臺灣大學<br>藥學研究所<br>88<br>This thesis is aimed to design and synthesize tryptanthrin and its analogs as potential anticancer agents. Tryptanthrin (1), indolo[2,1-b]quinazolin-6,12-dione, is a coplanar four-fused ring compound which contains N-phenylquinazoline skeleton similar to 2-phenylnaphthalene. It was illustrated that compounds containing coplanar 2-phenylnaphthalene skeletons exhibit different biological activities such as, ellipticine, camptothecin, while the bioactivities would be decreased or lost in unplanar structures. For example, batracylin, containing 2-phenyl-quinolone ske

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32

XU, GUO-RONG, and 吳國榮. "Synthetic studies on the dioxothia-analogues of pyrido [ 2,1-b ] quinazolin and rutaecarpine." Thesis, 1992. http://ndltd.ncl.edu.tw/handle/99012924338228446395.

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Wu, Guo-Rong, and 吳國榮. "Synthetic studies on the dioxothia-analogues of pyrido [ 2,1-b ] quinazolin and rutaecarpine." Thesis, 1992. http://ndltd.ncl.edu.tw/handle/65577392804971857510.

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34

Lo, Chi-Chun, and 羅吉鈞. "Synthesis and pharmacological evaluation of 4(3H)quinazolinone derivatives as potencial angiotensin II antagonists." Thesis, 1996. http://ndltd.ncl.edu.tw/handle/58461088283823970919.

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35

Li, Shi-Chen, and 李詩晨. "Part I、Design and synthesis of potential histone deacetylase inhibitorsPart II、Light-mediated synthesis of indazolo[3,2-b] quinazolines and their properties." Thesis, 2013. http://ndltd.ncl.edu.tw/handle/01094537045308387323.

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碩士<br>東海大學<br>化學系<br>102<br>Part I、Design and synthesis of potential histone deacetylase inhibitors This part of the thesis mainly described the design and attempted synthesis of the histone deacetylase inhibitors. First, we tried to react methyl 4-(3-hydroxyprop-1-yn-1-yl)-2-methoxybenzoate with tryptamine via a nucleophilic substitution reaction, but the yield was very low. Alternately, we tried to couple methyl 4-iodo-2-methoxybenzoate with propargyl bromide or allyl bromide using Sonogashira or Heck reaction, no desired products were obtained. Second, we switched the order of the synthesis

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36

Ho, Pei-Heng, and 何沛恒. "Design and Synthesis of Quinazolines Derivatives from Amino Acid Esters ; Copper-Catalysed Aerobic Oxidative Carbocyclization- Ketonization , Synthesis of Imidazo[1,2-a]benzimidazole Derivatives." Thesis, 2014. http://ndltd.ncl.edu.tw/handle/g4jy2w.

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37

Lai, Chi-Yuh, and 賴奇裕. "Total Synthesis of Fused Benzodiazepine and Quinazolinone Alkaloids: Circumdatin F, Ent-Fumiquinazoline Gand Their Analogs." Thesis, 2006. http://ndltd.ncl.edu.tw/handle/15537648530706358972.

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碩士<br>國立中正大學<br>化學所<br>95<br>Ent-fumiquinazoline G and its analogs contain unique structural motifs of quinazolinone and diketopiperazin-like skeletons. The key steps involved the intramolecular dehydration of a tripeptide derivative using triphenylphosphine, iodine, and DIEA and a final cyclization-upon-deprotection leading to the establishment of the desired products. Sixteen fumiquinazoline analogs were successfully prepared in our laboratory, the results reveal that piperazine motif of compounds having two side chains required longer reaction time than those having only one stereogenic ce

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38

Hour, Mann-Jen, and 侯曼貞. "Synthesis, Cytotoxicity and Antiplatelet Activity of 6,7,2',3',4',5'-Substituted 2-phenyl-4-quinazolinone Derivatives." Thesis, 2000. http://ndltd.ncl.edu.tw/handle/66215076548891573814.

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博士<br>中國醫藥學院<br>藥物化學研究所<br>88<br>As part of our continuing search for potential anticancer candidates of 2-phenyl-4-quinazolinones and 2-phenyl-4-quinolones, two series of 6,7,2',3',4',5'-substituted 2-phenyl-4-quinazolinones and 6,2',3',4',5'-substituted 2,3-dihydro-2-phenyl-4-quinazolinones have been synthesized and evaluated for cytotoxicity and inhibition of tubulin polymerization. Through these biological screening, a preliminary structure-activity relationship has been established. On the whole, a good correlation was found between the two activities. Among them, 6-N,N-dimethylamino and

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39

Liu, Chih-Fa, та 劉誌發. "design and synthesis of quinazolinone and 1,2-benzothiazine 1,1-dioxide derivatives as potential selective α1A-adrenoceptor antagonists". Thesis, 2000. http://ndltd.ncl.edu.tw/handle/59531007520783388600.

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碩士<br>國立臺灣大學<br>藥學研究所<br>88<br>This study is aimed to synthesize two series of compounds, namely, substituted arylpiperazinyl benzothiazinone 1,1-dioxide (A) and substituted arylpiperazinyl quinazolinone (B) derivatives for evaluation of α1A adrenoceptor selectivity and are considered to be potential for treatment of benign prostatic hyperplasia (BPH). The synthesis of compounds in A series started from esterification of 3,4-dimethoxyphenyl acetic acid (25) in methanol with a catalytic amount of concentrated sulfuric acid to give 3,4-dimethoxy-1-(carbomethoxymethyl)benzene (26). T

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Salahi, Rashad al [Verfasser]. "Synthesis of novel 2-alkoxy(aralkoxy)-4H-[1,2,4]triazolo[1,5-a]quinazolin-5-ones and derivatives / by Rashad Al-salahi." 2009. http://d-nb.info/993198538/34.

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Paumo, Hugues Kamdem. "2-Aryl-6,8-Dibromo-4-Chloroquinazoline as scaffold for the synthesis of Novel 2,6,8-Triaryl-4-(Phenylethynyl)Quinazolines with potential photophysical properties." Diss., 2014. http://hdl.handle.net/10500/14197.

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The 2-aryl-6,8-dibromoquinazolin-4(3H)-ones were prepared in a single-pot operation by condensing 6,8-dibromoanthranilamide and aryl aldehydes in the presence of molecular iodine in ethanol. Treatment of the 2-aryl-6,8-dibromoquinazolin-4(3H)-ones with thionylchloride in the presence of dimethylformamide afforded the corresponding 2-aryl-4-chloro-6,8-dibromoquinazolines. Palladium(0)-copper iodide catalysed Sonogashira cross-coupling reaction of 2-aryl-4-chloro-6,8-dibromoquinazolines with terminal alkynes at room temperature afforded series of 2-aryl-6,8-dibromo-4-(alkynyl)quinazolines. Furth

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Mmonwa, Mmakwena Modlicious. "Synthesis of Polyaryl-substituted Bisquinazolinones with potential photophysical properties." Diss., 2014. http://hdl.handle.net/10500/18789.

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3,5-Dibromo-2-aminobenzamide was reacted with 1,3-cyclohexanedione derivatives in the presence of iodine as catalyst in toluene under reflux to afford novel 6,8-dibromo-2-[3-(2´-alkyl-1´,2´,3´,4´-tetrahydro-6´,8´-dibromo-4´-oxoquinazoline-2yl)propyl]quinazolin-4(3H)-ones in high yields. Suzuki-Miyaura cross-coupling of the latter with arylboronic acids in the presence of Pd(PPh3)2Cl2–Xphos catalyst complex and K2CO3 as a base in dioxane-water mixture (3:1, v/v) afforded the corresponding polyaryl-substituted bis-heterocycles in a single step operation. The resultant compounds were characterize

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Yang, Huei-Yun, and 楊慧筠. "1.Lewis Acid-Mediated Total Synthesis of Quinazolinone Alkaloids and Their Analogs2.Study toward DNA-Protein Interactions Using Functionalized Ionic Liquids." Thesis, 2008. http://ndltd.ncl.edu.tw/handle/63287336302473943622.

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碩士<br>國立中正大學<br>化學所<br>97<br>Abstract There are two project in this thesis. The first project is “ Lewis Acid-Mediated Total Synthesis of Quinazolinone Alkaloids and Their Analogs ” . The previously reported methodologies for preparation of quinazolinone analogous , either required a number of synthetic steps or proceed with long reaction hours and low to moderate yields. In this thesis, Lewis acid and microwaves were employed to assist double cyclizations of tripeptide precursors to afford the total synthesis of quinazolinone analogs. At first, sclerotigenin, a natural product, was sele

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Yang, Ping-Syun, and 楊凭勲. "Part I: Rational Design and Synthesis of Tetrahydroisoquinoline- and Indole-Quinazolinone Conjugate with Anticancer Activities；Part II: Synthesis and Development of meta-Hydroxypyridines with Hypervalent Iodine (III) mediated Oxidative Coupling Reaction." Thesis, 2015. http://ndltd.ncl.edu.tw/handle/6rma65.

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博士<br>國立中山大學<br>化學系研究所<br>103<br>In this thesis, there are two parts in this dissertation. Part I: we have designed and synthesized a series of new generation of protenial anti-cancer drugs containing two biologically active structure tetrahydroisoquinoline and quinazolone, CWO compounds. CWO series of compounds, especially in 0-CWO, which has the best of the anti-cancer activity for IC50 (0.26 μM in MDA-MB-231 breast adenocarcinoma cells), and was found in apoptosis experiments have the results of early and late apoptotic cells. In addition, I also have synthesized a series of hetero-atom aro

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