Dissertations / Theses on the topic 'Late functionalization'
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Brown, Alec Nathaniel. "Late-Stage Functionalization of 1,2-Dihydro-1,2-Azaborines." Thesis, Boston College, 2015. http://hdl.handle.net/2345/bc-ir:104564.
Full textDescribed herein are two distinct research projects focused on the development of metal-catalyzed late-stage functionalization strategies for 1,2-dihydro-1,2-azaborines separated into three chapters. The first chapter discusses the development, synthesis, and recent contributions to the field of azaborine chemistry. The second chapter details the development of rhodium catalyzed B-H bond activation for the synthesis of a new class of BN-stilbenes as well as the discovery of a novel B-H to B-Cl transformation that is successful both with B-H azaborines as well as other B-H containing compounds. The third chapter pertains to the development of a B-H and B-Cl tolerant C(3) functionalization strategy through the use of Negishi cross-coupling. Using this methodology, previously unreported isomers of BN-naphthalene and BN-indenyl have been synthesized and characterized
Thesis (PhD) — Boston College, 2015
Submitted to: Boston College. Graduate School of Arts and Sciences
Discipline: Chemistry
Canelli, Tommaso. "Development of tandem C-H borylation/functionalization procedures for late stage functionalization of compounds." Master's thesis, Alma Mater Studiorum - Università di Bologna, 2015. http://amslaurea.unibo.it/9273/.
Full textBentley, Sierra Kathleen. "Selective Direct Borylation and Late-Stage Functionalization of 1,2-Azaborines:." Thesis, Boston College, 2020. http://hdl.handle.net/2345/bc-ir:109014.
Full textDescribed herein is the development of a method to directly borylate the C5-position of monocyclic 1,2-azaborines without the use of a metal catalyst, kinetic resolution or directing group. This method tolerates different substitution on the boron as well as at the C3-position of the azaborine. A new BN-isostere of the drug molecule, felbinac, was synthesized to demonstrate the application of this method
Thesis (MS) — Boston College, 2020
Submitted to: Boston College. Graduate School of Arts and Sciences
Discipline: Chemistry
Kaplaneris, Nikolaos [Verfasser]. "Resource-Economical C–H Activation for Late-Stage Functionalization / Nikolaos Kaplaneris." Göttingen : Niedersächsische Staats- und Universitätsbibliothek Göttingen, 2021. http://d-nb.info/1237128854/34.
Full textArmand, Jeremy Richard. "Late Stage Functionalization of 1,2-Azaborines for Application in Biomedical Research:." Thesis, Boston College, 2019. http://hdl.handle.net/2345/bc-ir:108646.
Full textChapter 1. Use of boron as a pharmacophore is as growing but still underdeveloped strategy for expanding chemical space in biomedical research. In addition to more established methods of incorporating boron in drug development, an attractive and emerging method of introducing boron into biologically active compounds is through boron-nitrogen containing heterocycles. In particular, the Liu group has focused on exploring the interactions of monocyclic 1,2-azaborines in biological space. In order to install complicated chemical functionality needed for further studies, methods for late stage functionalization of 1,2-azaborines must be developed. Described herein is a method for functionalizing 1,2-azaborine at the C3- and C5-positions, with bromine and iodine handles, respectively. Chapter 2. Described is the application of the turbo Grignard reaction to 1,2-azaborines bearing a B–Cl bond. The reaction utilizes iPrMgCl·LiCl to form aryl carbon nucleophiles and is tolerant of sensitive functional groups such as nitriles and esters. Development of the reaction obviates the need to use toxic organotin reagents to install aryl groups at the B-position that bear sensitive, electrophilic functionalities
Thesis (MS) — Boston College, 2019
Submitted to: Boston College. Graduate School of Arts and Sciences
Discipline: Chemistry
Chan, Jessica Zee. "Stereoselective Functionalization of Carbonyl Compounds and N-Alkylamines Promoted by Cooperative Catalysts:." Thesis, Boston College, 2020. http://hdl.handle.net/2345/bc-ir:108940.
Full textThis dissertation describes the development of cooperative catalyst systems for the functionalization of monocarbonyl compounds and stereoselective transformations of alpha-C–H bonds of N-alkylamines, inspired by the concepts of frustrated Lewis pairs (FLPs). Prior to this dissertation research, practical and broadly applicable C–C and C–heteroatom bond forming reactions involving the FLP complexes that provide synthetically desirable products with high enantioselectivity remained to be developed. Chapter 1 of this dissertation describes the recent advances in the transformations involving FLPs and B(C₆F₅)₃-catalyzed reactions. Inspired by the unique capability of FLP catalysts to activate otherwise unreactive molecules, and circumvent undesirable acid–base complexation, we have developed potent cooperative acid/base catalysts for C–C bond forming reactions of various monocarbonyl compounds and an appropriate electrophile, which will be discussed in Chapter 2. Another reactivity of FLPs to be explored has to do with the catalytic and enantioselective reactions of N-alkylamines, where two Lewis acid catalysts with potentially overlapping functions, work cooperatively to activate alpha-amino C–H bonds and promote the enantioselective C–C bond forming reaction between N-alkylamines and a nucleophilic species. In Chapter 3, B(C₆F₅)₃-catalyzed union of N-alkylamines and silicon enolates followed by the enantioselective B(C₆F₅)₃/Mg–PyBOX-catalyzed alpha-alkylation of N-alkylamines and alpha,beta-unsaturated compounds to form beta-amino carbonyl compounds will be described. In Chapter 4, B(C₆F₅)₃/Cu–PyBOX-catalyzed alpha-C–H alkynylation of N-alkylamines and the applications in late-stage functionalization and stereoselective synthesis will be discussed
Thesis (PhD) — Boston College, 2020
Submitted to: Boston College. Graduate School of Arts and Sciences
Discipline: Chemistry
Schischko, Alexandra. "Late-Stage Peptide Functionalization by Ruthenium-Catalyzed C H Arylations and Alkylations." Doctoral thesis, Niedersächsische Staats- und Universitätsbibliothek Göttingen, 2018. http://hdl.handle.net/11858/00-1735-0000-002E-E4F4-0.
Full textZhang, Zhuan. "Late Stage Modifications of Phosphines using Transition-Metal-Catalyzed C–H Bond Functionalization." Thesis, Rennes, Ecole nationale supérieure de chimie, 2020. http://www.theses.fr/2020ENCR0067.
Full textThe main objective of this PhD thesis deals with the preparation of polyfunctional phosphines by late-stage diversification of commercially available ligands. We have developed rhodium(I)-catalyzed ortho’- C–H bond alkylation of biarylphosphines. This new methodology provides a straightforward access to a large library of multifunctionalized phosphines. Some of these modified ligands outperformed commercially available phosphines in the Pd-catalyzed carboxylation of aryl bromides with carbon dioxide in the presence of a photoredox catalyst. To improve the diversity of biarylphosphines, we have also perfected the P(III)-directed C−H bond alkenylation of (dialkyl)- and (diaryl)biarylphosphines using internal alkynes. Chloride-free [Rh(OAc)(COD)]2 acts as a better catalyst than [RhCl(COD)]2. Conditions were developed to control the mono- and difunctionalization. One of these novel bisalkenylated (dialkyl)biarylphosphines was employed for the preparation of a palladium(II) complex, and some of these functionalized ligands outperformed their corresponding unfunctionalized phosphines in Pd-catalyzed amidation of sterically hindered aryl chlorides. Finally, we have also explored a novel protocol C–H bond alkylation of phosphines via 5- or 7- membered ring cyclometallated phosphineruthenium intermediates. These functionalized phosphines have potential to improve crosscoupling reactions of sterically hindered aryl (pseudo)halides
Poudel, Dhruba P. "Late-Stage Modification of Polyurethane Dendrimers Using Click Chemistry." Miami University / OhioLINK, 2021. http://rave.ohiolink.edu/etdc/view?acc_num=miami1627490978861964.
Full textHanson, Susan Kloek. "Synthesis and reactivity studies of late transition metal complexes relevant to C-H bond activation and functionalization /." Thesis, Connect to this title online; UW restricted, 2007. http://hdl.handle.net/1773/8631.
Full textBörgel, Jonas Verfasser], Tobias [Akademischer Betreuer] Ritter, and Franziska [Akademischer Betreuer] [Schönebeck. "Late-stage functionalization of arenes: from C-H amination to C-H oxygenation and deoxyfluorination / Jonas Börgel ; Tobias Ritter, Franziska Schoenebeck." Aachen : Universitätsbibliothek der RWTH Aachen, 2019. http://d-nb.info/121086293X/34.
Full textSang, Ruocheng Verfasser], Tobias [Akademischer Betreuer] Ritter, and Carsten [Akademischer Betreuer] [Bolm. "Late-stage functionalization of arenes: site-selective C-H oxygenation and fluorination via aryl sulfonium salts / Ruocheng Sang ; Tobias Ritter, Carsten Bolm." Aachen : Universitätsbibliothek der RWTH Aachen, 2020. http://d-nb.info/1221697455/34.
Full textBöhm, Marvin Jeldrik. "Synthesis and reactivity of succinylthioimidazolium salts: A unified strategy for the preparation of thioethers." Doctoral thesis, Niedersächsische Staats- und Universitätsbibliothek Göttingen, 2020. http://hdl.handle.net/21.11130/00-1735-0000-0005-152E-1.
Full textZhu, Yingjun. "Sustainable Strategies for Site-Selective C–H Functionalizations of N-Heterocycles." Doctoral thesis, Niedersächsische Staats- und Universitätsbibliothek Göttingen, 2015. http://hdl.handle.net/11858/00-1735-0000-0022-5DDA-D.
Full textLeroux, Marcel Rainer [Verfasser], and Paul [Akademischer Betreuer] Knochel. "Late-stage functionalization of peptides and cyclopeptides using organozinc reagents and pyrrole protected 2-Aminoalkylzinc reagents for the enantioselective synthesis of amino derivatives / Marcel Rainer Leroux ; Betreuer: Paul Knochel." München : Universitätsbibliothek der Ludwig-Maximilians-Universität, 2020. http://d-nb.info/1208150057/34.
Full textSchischko, Alexandra [Verfasser], Lutz [Akademischer Betreuer] Ackermann, Lutz [Gutachter] Ackermann, Dietmar [Gutachter] Stalke, Manuel [Gutachter] Alcarazo, Franziska [Gutachter] Thomas, Shoubhik [Gutachter] Das, and Alexander [Gutachter] Breder. "Late-Stage Peptide Functionalization by Ruthenium-Catalyzed C H Arylations and Alkylations / Alexandra Schischko ; Gutachter: Lutz Ackermann, Dietmar Stalke, Manuel Alcarazo, Franziska Thomas, Shoubhik Das, Alexander Breder ; Betreuer: Lutz Ackermann." Göttingen : Niedersächsische Staats- und Universitätsbibliothek Göttingen, 2018. http://d-nb.info/1170955819/34.
Full textMamontov, Alexander. "Hydroxylation et halogénation directe et sélective des composés azotés en milieu superacide." Thesis, Poitiers, 2018. http://www.theses.fr/2018POIT2267.
Full textLate-stage functionalization can now be considered as a synthetic tool of choice to create molecular diversity, especially in a medicinal chemistry context. For example, aromatic C-H bonds can be regarded as functional groups and points of potential diversification to generate new analogs of a lead structure without resorting to de novo synthesis.The direct functionalization of elaborated compounds can also be done using superacid chemistry as demonstrated by the previous work of professor Jacquesy. One of the best examples of this strategy is certainly the direct transformation of vinorelbine (Navelbine®) by fluorination in superacid conditions to lead to its difluorinated analogue (Vinflunine), marketed by Pierre Fabre laboratories as an anticancer agent Javlor®.In this context, these studies focused on the development of new methods for the direct functionalization of aromatic nitrogen containing compounds.In particular, this work aimed at developing new synthetic tools in superacid for:1. the direct hydroxylation of aromatic compounds;2. the halogenation of aromatic nitrogen compounds from simple anilines to naturally occurring or synthetic compounds;3. the synthesis of labelled compounds with stable isotopes
Panza, Florian. "Fοnctiοnnalisatiοn directe οrthοgοnale métallο-catalysée des sites carbοne-hydrοgène des platefοrmes pharmacοlοgiques à cοeur imidazοisοindοle." Electronic Thesis or Diss., Normandie, 2024. http://www.theses.fr/2024NORMIR11.
Full textFor several decades, chemists constantly seek to push the limits of synthetic strategies by developing ever more efficient and more economical methodologies. In this context, transition metal-catalyzed direct functionalization of C—H bonds is one of the most powerful tools for constructing and funtionalizing simple molecules and ever more complex moieties, with a great diversity of C—H bonds. These strategies also answer the needs for the opening of the chemical space of functionalization. Imidazoisoindole, tricyclic heterocycle composed of an imidazole core, is a very interesting scaffold for biological activity and presents C—H bonds with very diverse properties, but late-functionalization methodology of these structures has yet to be listed in the literature. This work takes place in this context and presents, (I) based on past laboratory experience, a robust methodology to synthetize diversely substituted imidazoisoindoles at high scale by palladium-catalyzed intramolecular C—H activation ; (II) an extension of standard directC2—H functionalization of 1,3-diazole moieties applied to imidazo[5,1-a]isoindoles with a palladium(0)-copper(I) cooperative catalysis ; (III) a new methodology of direct C(sp³)—H palladium-catalyzed mono-functionalization at benzylic position of imidazo[2,1-a]isoindoles ; (IV) a preliminary study of the observed regioselectivity of iridium-catalyzed direct C(sp²)—H borylation of imidazo[2,1-a]isoindoles
Zakis, Janis Mikelis. "Catalyseurs d'iridium cyclométallés pour la borylation ortho-dirigée de C–H." Electronic Thesis or Diss., Strasbourg, 2024. http://www.theses.fr/2024STRAF006.
Full textC–H borylation has continued to evolve from early examples of stoichiometric reactions to a method employed for building block synthesis on a kilogram scale. However, challenges remain for its wider application. We have developed new bis-cyclometallated iridium complexes exhibiting an improved reactivity and air-stability. These complexes have been used for the ortho-directed C–H borylation of arenes, heterocycles, and acrylamides, achieving average to high yields. By combining these new catalysts with high-throughput screening, we rapidly evaluated the reactivity of different directing groups, enabling predictions for the functionalization of substrates with multiple directing groups. Mechanistic studies revealed the details how these new bis-cyclometallated complexes are activated during the reaction. Subsequently, we investigated ligand free borylation and found a wide range of compatible substrates. We then investigated miniaturization of C-H borylation reactions and successfully conducted them on micromolar scale. By integrating our findings with those from the literature, we designed a screening platform comprising eight different reaction conditions. This platform was used to screen a vast array of small molecules, as well as more complex substrates. The results revealed differences between the catalytic systems and allowed us to successfully functionalize complex molecules. These findings highlight the widespread of ligand-free borylation as well as the limitations of the current state-of-the-art methods
Jamshaid, Talha. "Synthèse de latex magnétique submicronique et fonctionnalisé pour application en biocapteur." Thesis, Lyon, 2016. http://www.theses.fr/2016LYSE1061/document.
Full textObjective of this work is to overcome all those tedious and time consuming processes likefiltration and centrifugation which are used in in-vitro applications. Moreover, suchparticles which are suitable for use in lab-on-a-chip and biosensors systems are produced.Submicron magnetic latex particles (MLPs) with desired core-shell morphology wereprepared. Oil in water (o/w) magnetic emulsion (home-made) was used as seed of radicalemulsion polymerization of Styrene (St.) as a monomer and cross-linker divenylbenzene (DVB ) in the presence of potassium persulfate (KPS) and 4, 4'-azobis cyanopentanoic acid(ACPA) as an initiators. Particles surface was functionalized with sulfate and carboxylicgroups by using the initiators.A novel capacitance electrochemical biosensor based on silicon nitride substrate (Si3N4)combined with MLPs was developed. MLPs with terminated carboxylic acid werecovalently bonded to Si3N4 through a Self-Assembled Monolayers (SAMs) of the silaneamine(3- Aminopropyl) triethoxysilane (APTES). Finally anti-ochratoxin A antibodieswere immobilized on MLPs by amide bonding. Electrochemical measurements werecarried out using Mott-Schottky analysis for ochratoxin A (OTA) detection.Using application of competitive assay through immobilized fixed concentration of antigen (SA2BSA)and antibody (Ab 155) respectively was measured against different concentrations of sulfa pyridine(SPY), with and without use of MLPs with carboxylic group functionality. Biosensor sensitivityincreased, when MLPs were used
LENCI, ELENA. "Diversity-Oriented Synthesis of novel glyco- and peptidomimetic scaffolds." Doctoral thesis, 2017. http://hdl.handle.net/2158/1091042.
Full textZheng, Lei. "Noncovalent Functionalization of Latex Particles using High Molecular Weight Surfactant for High-Performance Coatings." 2019. https://scholarworks.umass.edu/masters_theses_2/813.
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