Дисертації з теми "Total Synthesis, Antibiotics"
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Preece, Lewis. "Studies toward a total synthesis of Lactonamycin." Thesis, University of Sussex, 2012. http://sro.sussex.ac.uk/id/eprint/39607/.
Повний текст джерелаWohlrab, Aaron M. "The total synthesis of depsipeptide antibiotics." Connect to a 24 p. preview or request complete full text in PDF format. Access restricted to UC campuses, 2007. http://wwwlib.umi.com/cr/ucsd/fullcit?p3284214.
Повний текст джерелаTitle from first page of PDF file (viewed January 14, 2008). Available via ProQuest Digital Dissertations. Vita. Includes bibliographical references.
Lineswala, Jayana P. "Total synthesis of lavendamycin amides." Virtual Press, 1996. http://liblink.bsu.edu/uhtbin/catkey/1036197.
Повний текст джерелаDepartment of Chemistry
Martin, Bruce John. "A total synthesis of myxothiazol." Thesis, University of Nottingham, 1994. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.283643.
Повний текст джерелаGlover, Christian. "Towards the total synthesis of thiopeptide antibiotics." Thesis, Cardiff University, 2006. http://orca.cf.ac.uk/56094/.
Повний текст джерелаKarki, Rajesh. "Total synthesis of oxygenated lavendamycin analogs." Virtual Press, 1998. http://liblink.bsu.edu/uhtbin/catkey/1115420.
Повний текст джерелаDepartment of Chemistry
Chen, Deqi. "Studies towards the total synthesis of aerocyanidin." Thesis, University of Oxford, 1994. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.240567.
Повний текст джерелаWard, Richard Anthony. "A total synthesis of AI-77-B." Thesis, University of Salford, 1992. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.315364.
Повний текст джерелаStocksdale, Mark G. "Total synthesis of lavendamycin analogs." Virtual Press, 1992. http://liblink.bsu.edu/uhtbin/catkey/834647.
Повний текст джерелаDepartment of Chemistry
Chenault, Darrell Vincent. "Total synthesis of 6-chlorodemethyllavendamycin esters and amides." Virtual Press, 1998. http://liblink.bsu.edu/uhtbin/catkey/1115748.
Повний текст джерелаDepartment of Chemistry
Freeman, Richard Neil Templar. "The total synthesis of non-beta-lactam antibiotics." Thesis, University of Oxford, 1990. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.257963.
Повний текст джерелаRawson, D. J. "A total synthesis of (+)-(9S)-dihydroerythronolide A." Thesis, University of Cambridge, 1989. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.317889.
Повний текст джерелаOlang, Fatemeh. "Total synthesis of lavendamycin analogs." Virtual Press, 1995. http://liblink.bsu.edu/uhtbin/catkey/958797.
Повний текст джерелаDepartment of Chemistry
Fellows, Ingrid Maria. "A formal synthesis of FR-900482 and studies toward the total synthesis of FR-900482 /." Digital version accessible at:, 1999. http://wwwlib.umi.com/cr/utexas/main.
Повний текст джерелаHe, Jing. "Studies towards the total synthesis of tetrodecamycin." Thesis, University of Oxford, 2007. http://ora.ox.ac.uk/objects/uuid:3a2ab5cb-2757-4e53-b8cf-c635aef99455.
Повний текст джерелаLi, Chengyong, and 李成永. "Total syntheses (-)-5-demethoxyfumagillol, (-)-fumagillol, (-)-RK-805,(-)-FR65814, and analogues." Thesis, The University of Hong Kong (Pokfulam, Hong Kong), 2008. http://hub.hku.hk/bib/B39793977.
Повний текст джерелаBasu, Shubhamita. "STUDIES TOWARDS THE TOTAL SYNTHESIS OF VANCOMYCIN AGLYCON." Case Western Reserve University School of Graduate Studies / OhioLINK, 2007. http://rave.ohiolink.edu/etdc/view?acc_num=case1183157258.
Повний текст джерелаStansfield, Ian. "Synthetic and modelling studies on macrolide antibiotics : total synthesis of novel analogues of erythromycin A." Thesis, University of Cambridge, 1995. https://www.repository.cam.ac.uk/handle/1810/271994.
Повний текст джерелаAbou, Fayad Antoine. "Combining synthesis and biosynthesis to generate novel antibiotics." Thesis, University of St Andrews, 2014. http://hdl.handle.net/10023/6359.
Повний текст джерелаVickers, Clare Frances. "A study concerning the total synthesis of the natural products abyssomicin C and stemofoline." Thesis, University of Manchester, 2008. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.491851.
Повний текст джерелаBurnside, I. J. "Synthetic studies on macrolide antibiotics : the total synthesis of (+)-(6R)-Fluoro-6-deoxy-(9S)-dihydroerythronolide A." Thesis, University of Cambridge, 1996. https://www.repository.cam.ac.uk/handle/1810/273078.
Повний текст джерелаGlassford, Ian Michael. "Addressing Antibiotic Resistance: The Discovery of Novel Ketolide Antibiotics Through Structure Based Design and In Situ Click Chemistry." Diss., Temple University Libraries, 2016. http://cdm16002.contentdm.oclc.org/cdm/ref/collection/p245801coll10/id/410231.
Повний текст джерелаPh.D.
Antibiotic resistance has become and will continue to be a major medical issue of the 21st century. If not addressed, the potential for a post-antibiotic era could become a reality, one that the world has not been familiar with since the early 1900’s. Multidrug-resistant hospital-acquired bacterial infections already account for close to 2 million cases and 23,000 deaths in the United States, along with 20 billion dollars of additional medical spending each year. The CDC released a report in 2013 regarding the seriousness of antibiotic resistance and providing a snapshot of costs and mortality rates of the most serious antibiotic resistant bacteria, which includes 17 drug resistant bacteria, such as carbapenem-resistant Enterobacteriaceae, vancomycin-resistant Enterococcus and Staphylococcus aureus, and multidrug-resistant Acinetobacter and Pseudomonas aeruginosa. The development of antibiotic resistance is part of bacteria’s normal evolutionary process and thus impossible to completely stop. To ensure a future where resistant bacteria do not run rampant throughout society, there is a great need for new antibiotics and accordingly, methods to facilitate their discovery Macrolides are a class of antibiotics that target the bacterial ribosome. Since their discovery in the 1950’s medicinal chemistry has created semi-synthetic analogues of natural product macrolides to address poor pharmacokinetics and resistance. Modern X-Ray crystallography has allowed the chemist access to high resolution images of the bacterial ribosome bound to antibiotics including macrolides which has ushered in an era of structure-based design of novel antibiotics. These crystal structures suggest that the C-4 methyl group of third generation ketolide antibiotic telithromycin can sterically clash with a mutated rRNA residue causing loss of binding and providing a structural basis for resistance. The Andrade lab hypothesized that the replacement of this methyl group with hydrogen would alleviate the steric clash and allow the antibiotic to retain activity. To this end, the Andrade lab set out on a synthetic program to synthesize four desmethyl analogues of telithromycin by total synthesis that would directly test the steric clash hypothesis and also provide structure-activity relationships about these methyl groups which have not been assessed in the past. Following will contain highlights of the total synthesis of (-)-4,8,10-didesmethyl telithromycin, (-)-4,10-didesmethyl telithromycin, and (-)-4,8-desmethyl telithromycin and my journey toward the total synthesis of (-)-4-desmethyl telithromycin Traditional combinatorial chemistry uses chemical synthesis to make all possible molecules from various fragments. These molecules then need to be purified, characterized, and tested against the biological target of interest. While high-throughput assay technologies (i.e., automation) has streamlined this process to some extent, the process remains expensive when considering the costs of labor, reagents, and solvent to synthesize, purify, and characterize all library members. Unlike traditional combinatorial chemistry, in situ click chemistry directly employs the macromolecular target to template and synthesize its own inhibitor. In situ click chemistry makes use of the Huisgen cycloaddition of alkyne and azides to form 1,2,3-triazoles, which normally reacts slowly at room temperature in the absence of a catalyst. If azide and alkyne pairs can come together in a target binding pocket the activation energy of the reaction can be lowered and products detected by LC-MS. Compounds found in this way generally show tighter binding than the individual fragments. Described in the second part of this dissertation is the development of the first in situ click methodology targeting the bacterial ribosome. Using the triazole containing third generation ketolide solithromycin as a template we were able to successfully show that in situ click chemistry was able to predict the tightest binding compounds.
Temple University--Theses
O'Riordan, Timothy Jeremiah Cornelius. "Synthesis of the pyrrolidinone core of oxazolomycin A." Thesis, University of Oxford, 2009. http://ora.ox.ac.uk/objects/uuid:298746d3-69df-47b9-8a83-7949df1c94dc.
Повний текст джерелаWildermuth, Raphael [Verfasser], and Thomas [Akademischer Betreuer] Magauer. "A modular synthesis of tetracyclic meroterpenoid antibiotics : towards the total synthesis of cornexistin / Raphael Wildermuth ; Betreuer: Thomas Magauer." München : Universitätsbibliothek der Ludwig-Maximilians-Universität, 2018. http://d-nb.info/1222908905/34.
Повний текст джерелаBaker, Simon. "Studies towards the total synthesis of BU-4794F and alkene metathesis in the synthesis of novel β-lactam antibiotics." Thesis, Imperial College London, 2000. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.326162.
Повний текст джерелаBułyszko, Ilona [Verfasser]. "Studies on ansamycin antibiotics : mutasynthetic approach towards new rifamycin derivatives and total synthesis of progeldanamycin derivatives / Ilona Bułyszko." Hannover : Technische Informationsbibliothek (TIB), 2016. http://d-nb.info/1126666726/34.
Повний текст джерелаCascales, Jiménez Víctor. "Síntesis total de la Anfidinolida B(2)." Doctoral thesis, Universitat de Barcelona, 2021. http://hdl.handle.net/10803/673064.
Повний текст джерелаIn this Thesis we have undertaken the total synthesis of Amphidinolide B2, a 25-membered macrolide. It was first isolated by Shimizu and coworkers in 1994, from Brewer’s Bay, Saint Thomas, one of USA’s Virgin Islands. This molecule has a very interesting structure and an important cytotoxicity. Carter’s proposal of the structure of Amphidinolide B2 has yet to be confirmed, so that the total synthesis of this macrolide becomes an attractive goal. Our proposal for the synthesis of this molecule is based on the disconnection of the macrocycle into four, more simple, Fragments. In Chapter 2 the preparation of Fragment I was optimized, as the previously developed syntheses were relatively unsuccessful. Six different routes were studied for the preparation of ketone 10, a key intermediate in our synthesis. Finally, Fragment I was obtained in six steps, in a 44% yield starting from methyl-diethyl malonate. In Chapter 3 we approached the synthesis of Fragment II. Originally, we optimized a previous synthesis developed in group for this Fragment, obtaining the desired compound in 11 steps and a 17% yield starting from (S)-methyl lactate. Due to the high number of steps of this route, we explored two alternatives. However, both were unsuccessful. Fragment III was prepared in Chapter 4, following a retrosynthesis previously described in our group. However, discouraging results were obtained in the initial transformations, which made us search for a new route. In the end, Fragment III was obtained in six steps and in a 52% yield starting from butane-1,4-diol. The preparation of a shortened version of Fragment IV is described in Chapter 5, following a previous retrosynthesis. Because an intermediate step proved troublesome, a new approximation was studied, with no success. Finally, Fragment IV was prepared in three steps and in a 44% yield starting from 2,3-dibromopropene With the different Fragments in our hands, their coupling was investigated. Initially, we joined Fragment I with Fragment IV via a Negishi cross coupling. The obtained product was then transformed into the corresponding iodide, which was used in a second Negishi cross coupling. Despite our efforts, low yields were obtained in this transformation which also showed little reproducibility. Therefore, an alternative, promising route was investigated. After functional group manipulation, the desired epoxyaldehyde was prepared. Then, Fragment III was introduced via a Julia–Kocienski olefination. Hydrolysis of the ester, followed by a Shiina esterification was used to link Fragment II. At this moment, we are exploring the next step, the ring closing metathesis for the formation of the macrocycle.
Hayes, J. F. "Studies towards the total asymmetric synthesis of macbecin." Thesis, University of Southampton, 1986. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.374854.
Повний текст джерелаChan, Tsui Fen. "Studies towards the total synthesis of ambruticin." Thesis, University of Salford, 1997. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.244865.
Повний текст джерелаPapillon, Julien Pierre Nicolas. "Studies towards the asymmetric total synthesis of oxazolomycin." Thesis, University of York, 2002. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.288241.
Повний текст джерелаDymock, Brian William. "A novel asymmetric [2+2] cycloaddition and its application to the total synthesis of 1233A." Thesis, University of Glasgow, 1997. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.388549.
Повний текст джерелаAshcroft, Neil David. "Towards a total synthesis of the ansamycin antibiotic herbimycin A." Thesis, University of Reading, 1995. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.294580.
Повний текст джерелаPietsch, Inga-Marlene. "Studies towards the total synthesis of the ansamycin benzoquinone antibiotic herbimycin A." Thesis, University of Sussex, 2009. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.496799.
Повний текст джерелаKhatri, Hem Raj. "Synthesis of Complex ortho-Allyliodoarenes via Reductive Iodonio-Claisen Rearrangement and Total Synthesis of Antitumor Antibiotic Derhodinosylurdamycin A." University of Toledo / OhioLINK, 2015. http://rave.ohiolink.edu/etdc/view?acc_num=toledo1431342601.
Повний текст джерелаGuzman-Martinez, Aikomari. "Total synthesis of lysobactin a natural product antibiotic active against methicillin and vancomycin resistant bacteria /." Diss., Connect to a 24 p. preview or request complete full text in PDF format. Access restricted to UC campuses, 2007. http://wwwlib.umi.com/cr/ucsd/fullcit?p3284164.
Повний текст джерелаTitle from first page of PDF file (viewed January 11, 2008). Available via ProQuest Digital Dissertations. Vita. Includes bibliographical references.
Hemmery, Hélène. "Étude de la synthèse totale de la ripostatine A." Thesis, Paris 11, 2014. http://www.theses.fr/2014PA112336/document.
Повний текст джерелаThis thesis is dedicated to the study of the total synthesis of ripostatin A, an antibiotic which inhibits eubacterial RNA polymerase, isolated in 1995 from the myxobacteria Sorangium cellulosum. Ripostatin A is characterized by a 14 membered lactone and a 6 membered lactol, it contains three double bonds and three stereogenic centers. The two synthetic routes envisaged for ripostatin A included as key steps a nitrile oxide 1,3 dipolar cycloaddition and a macrolactonisation. Stereocontroled accesses to two important precursors containing a 1,4-diene moiety were developed, using in particular an alkyne carboalumination. Advanced precursors, β-hydroxyketones, were obtained from these 1,4 dienes. A Stille coupling between a synthesized stannane and an halide derived from one of the β-hydroxyketones, remains to be realized in order to assemble the skeleton of ripostatin A
George, Nicolas. "Étude de la synthèse totale de tétrahydroisoquinoléines naturelles : quinocarcine, Tétrazomine et Lémonomycine. : rapide accés aux α-amidosulfures et leur utilisation en tant que précurseurs de N-acylimines dans la réaction de Friedel-Crafts". Phd thesis, Université Paris Sud - Paris XI, 2011. http://tel.archives-ouvertes.fr/tel-00980348.
Повний текст джерелаTun, Min Min. "Synthetic studies towards the total synthesis of renieramycin A (Antibiotics)." Thesis, 1988. http://hdl.handle.net/1911/13323.
Повний текст джерелаHecker, Evan Adam 1980. "Studies toward the total synthesis of (±)-chartelline C and (-)-platensimycin." 2008. http://hdl.handle.net/2152/17858.
Повний текст джерелаtext
Norbeck, Daniel Word. "Progress Toward the Total Synthesis of Polyether Ionophore Antibiotics." Thesis, 1985. https://thesis.library.caltech.edu/11444/2/Norbeck_DW_1985.pdf.
Повний текст джерелаSeveral subunits for the convergent synthesis of polyether ionophore antibiotics via the ester enolate Claisen rearrangement of furanoid and pyranoid carboxylic acids and glycals are prepared from carbohydrates. Key steps from D-fructose to the monensin spiroketal include the ester enolate Claisen rearrangement of a glycal propionate, expansion of a furanoid to a pyranoid ring, and the acid catalyzed equilibration of a bicyclic ketal to a spiroketal. An alternative approach, entailing the hetero-Diels-Alder condensation of a 2-methylenetetrahydropyran and acrolein is thwarted by facile isomerization to the endocyclic enol ether. The monensin bis-tetrahydrofuran is prepared from D-xylose and Dmannose. In the key step, in situ silylation of an ester enolate with a beta leaving group allows the tetrahydrofuran rings to be joined by Claisen rearrangement. The monensin tetrahydropyran is prepared from D-fructose and then joined to the bis-tetrahydrofuran by the ester enolate Claisen rearrangement. Methodology for the radical induced, reductive decarboxylation of the resulting acid via its phenyl selenoester is described. Anomeric stabilization of the intermediate tetrahydrofuran-2-yl radical is an important factor in the stereochemical outcome of this process. Reduction of 2,3-Q-(1-methylethylidene)furanosyl and pyranosyl chloride with lithium 4,4'-di-t-butylbiphenyl affords the corresponding glycals in high yield. The direct addition of nucleophilic reagents to crude Swern oxidation reaction mixtures circumvents the deleterious side reactions characteristic of highly reactive carbonyl compounds. Hexylglyoxal, produced by Swern oxidation of 1,2-octanediol, condenses with methyl (triphenylphosphoranylidene)acetate to give the γ-oxo-crotonate. Addition of methyl magnesiun bromide to an unstable 2-ketofuranoside delivers the branched chain carbohydrate derivative. The transient existence of monomeric trimethylsilyl formaldehyde, generated at -78°C by Swern oxidation of trimethylsilylmethanol, is established by isolation of a Wittig condensation product.
Suttisintong, Khomson. "Studies toward the total synthesis of sanglifehrin A." Thesis, 2012. http://hdl.handle.net/1957/33199.
Повний текст джерелаGraduation date: 2013
O'Keefe, Brian Michael. "Synthetic studies on the pluramycin family of antitumor antibiotics : the total synthesis of isokidamycin." Thesis, 2010. http://hdl.handle.net/2152/ETD-UT-2010-12-2035.
Повний текст джерелаtext
Ghosh, Partha. "New methods and strategies towards total synthesis of (9S)-dihydroerythronolide A." 2008. http://hdl.rutgers.edu/1782.2/rucore10001600001.ETD.17316.
Повний текст джерелаMahapatra, Subham. "Part I: Total synthesis of marine macrolide amphidinolide F and synthetic studies toward amphidinolide C; Part II: Computational study on proline sulfonamide-catalyzed aldol reaction." Thesis, 2013. http://hdl.handle.net/1957/37033.
Повний текст джерелаGraduation date: 2013
Loong, David Tien Jack. "Stereoselective total syntheses of the macrolides (-)-cladospolide A and (+)-microcarpalide." Phd thesis, 2003. http://hdl.handle.net/1885/151275.
Повний текст джерелаCvengroš, Ján. "Metal based strategies for the total synthesis of the antibiotics pestalone and patulin and structural analogues /." 2006. http://digitool.hbz-nrw.de:1801/webclient/DeliveryManager?pid=2225000&custom_att_2=simple_viewer.
Повний текст джерела(6616715), Kwaku Kyei-Baffour. "DEVELOPMENT OF ARYL ISONITRILES AS ANTIMICROBIAL AGENTS, AND TOTAL SYNTHESIS OF 17-NOR-EXCELSINIDINE." Thesis, 2019.
Знайти повний текст джерела
Infectious diseases caused by bacteria, fungi, and plasmodium parasites are a huge global health problem which ultimately leads to millions of deaths annually. The emergence of strains that exhibit resistance to nearly every class of antimicrobial agents, and the inability to keep up with these resistance trends has brought to the fore the need for new therapeutic agents (antibacterial, antifungal, and antimalarial) with novel scaffolds and functionalities capable of targeting microbial resistance. A novel class of compounds featuring an aryl isonitrile moiety has been discovered that exhibits potent inhibitory activity against several clinically relevant strains of methicillin-resistant Staphylococcus aureus (MRSA). Synthesis, structure-activity relationship (SAR) studies, and biological investigations have led to lead molecules that exhibit anti-MRSA inhibitory activity as low as 1 – 2 µM. The most potent compounds have also been shown to have low toxicity against mammalian cells and exhibit in vivo efficacy in MRSA skin and thigh infection mouse models.
The novel aryl isonitriles have also been evaluated for antifungal activity. This study examines the SAR of aryl isonitrile compounds and showed the isonitriles as compounds that exhibit broad spectrum antifungal activity against species of Candida and Cryptococcus. The most potent derivatives are capable of inhibiting growth of these pathogens at concentrations as low as 0.5 µM. Notably, the most active compounds exhibit excellent safety profile and are non-toxic to mammalian cells up to 256 µM.
Beyond the antibacterial and antifungal activities, structure-antimalarial relationship analysis of over 40 novel aryl isonitrile compounds has established the importance of the isonitrile functionality as an important moiety for antimalarial activity. Of the many isonitrile compounds exhibiting potent antimalarial activity, two have emerged as leads with activity comparable to that of Artemisinin. The SAR details presented in this study will prove essential for the development new aryl isonitrile analogues to advance them to the next step in the antimalarial drug discovery process.
17-nor-Excelsinidine, a zwitterion monoterpene indole alkaloid isolated from Alstonia scholaris is a subject of synthetic scrutiny. This is primarily due to its intriguing chemical structure which includes a bridged bicyclic ammonium moiety, and its anti-adenovirus and anti-HSV activity. Herein we describe a six-step total synthesis of (±)-17-nor-Excelsinidine from tryptamine. Key to the success of this synthesis is the use of palladium-catalyzed carbonylative heck lactamization methodology which built the 6, 7-membered ring lactam in one step. The resulting pentacyclic product, beyond facilitating the easy access to (±)-17-nor-Excelsinidine, could also serve as a precursor to other related indole alkaloids.
Morrison, Christopher F. "Efforts directed towards an asymmetric total synthesis of the antitumor antibiotic Fredericamycin A and a study of the Diels-Alder reactions of a carvone-derived diene /." 2001.
Знайти повний текст джерелаDorich, Stéphane. "Progrès vers la synthèse totale de la Pactamycine." Thèse, 2008. http://hdl.handle.net/1866/7818.
Повний текст джерелаDorich, Stéphane. "Synthèse totale de la pactamycine et d’une sélection d’analogues, progrès vers la synthèse totale de la daphniglaucine C et brève étude d’une transposition allylique réductrice." Thèse, 2013. http://hdl.handle.net/1866/10129.
Повний текст джерелаAlthough pactamycin was first isolated as a potential antitumoral drug, further studies highlighted its capacities in inhibiting protein synthesis, and thus its potency as an antibacterial agent. Furthermore, it was recently discovered that some of its analogs display promising antiprotozoal activity. The present thesis reports and details the first total synthesis of pactamycin, pursued in the Hanessian lab over the last few years, as well as the preparation of a selection of analogs thereby tested for their biological properties. Daphniglaucin C belongs to a large family of natural compounds isolated from the leaves of daphniphyllum over the last decade. Although relatively little is known as to the biological activity of daphniglaucin C, its synthesis poses an obvious and interesting challenge for organic chemists. En route towards its total synthesis, the use of several methods for the formation of quaternary centers was explored. Moreover, an atypical reductive allylic transposition, catalyzed by palladium from unactivated allylic alcohols, was studied and used to generate a variety of polysubstituted pyrrolidines.