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Showing 1 to 20 of 84 for “"Arylation"”.
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Cysteine arylation
… goal of this thesis is to develop new cysteine arylation reactions to generate sulfur-sp² carbon bonds on proteins. These reactions are used to make novel peptide and protein therapeutics. Two mechanistically complementary approaches are developed to arylate cysteine thiol. First, through a …
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Long peptides for cysteine arylation
Biological reactivity is typically carried out by large enzymes. There are few examples of reactive, amino-acid-based polymers shorter than 100 residues in length. Of those that do exist, the majority are very short tags (<15 amino acids). Here, we attempted to first discover peptides roughly 30 …
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COPPER-MEDIATED N1-ARYLATION OF BENZOTRIAZOLES
… one-pot reaction was designed. After <em>N</em>-arylation was complete and without any further purification, the reduction step was performed using B<sub>2</sub>(OH)<sub>4</sub>in MeCN. The method proved beneficial for the reaction with phenylboronic acid, and no significant improvement was …
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Development and Mechanistic Investigation of the Palladium-Catalyzed Alpha-Arylation of Aldehydes and N-Arylation of Ammonia
A general method for the palladium-catalyzed coupling of ammonia with aryl halides and sulfonates was also developed. The catalyst generated from Pd[P(o-tol)3]2 and the alkylbisphophine CyPF-t-Bu is a highly active and selective catalyst for the coupling of ammonia with aryl chlorides, bromides, …
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Development and mechanistic investigation of the palladium-catalyzed α-arylation of aldehydes and N-arylation of ammonia
A general method for the palladium-catalyzed α-arylation of aldehydes was developed to couple linear and branched aldehydes with electron-poor and electron-rich bromo- and chloroarenes in high yields. Catalysts generated from allylpalladium chloride (APC) and 1,1’-diphenylphosphinoferrocene (DPPF) …
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The arylation of 2-pyrones and related heterocycles
… to 2-pyrones and related heterocycles. Direct arylation via C–H activation of 2-pyrone, 2-pyridone and 2-coumarin compounds is described in Chapter 2. Protocols for the palladium-catalysed direct arylation of these molecules were developed and applied to a library of substrates. C–H activation …
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Late stage oxidative C(sp3)–H alkylation and arylation
Submission published under a 24 month embargo labeled 'Closed Access', the embargo will last until 2024-05-01
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New Methods for Palladium-catalyzed Decarboxylative Benzylation, Arylation and Dearomatization Reactions
… catalytic decarboxylative dearomatization and arylation reactions of ketone enolates. Two sets of protocols involving simple variation of ligands were then developed for the selective decarboxylative dearomatization or arylation of enolates. These methods provided alicyclic and mono-α-arylated …
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Direct arylation of 2-pyrones, coumarins, 2-pyridinones and 2-quinolones
Direct arylation via C-H activation displays a number of advantages over traditional (Suzuki-Miyaura, Stille, etc.) coupling reactions. The 2-pyrone, coumarin, 2-pyridinone and 2-quinolone moieties are prevalent in numerous compounds which exhibit biological activity. In addition, due to the varied …
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Chloro-arylation of Alkenes via Cooperative Photoredox and Atom-transfer Catalysis
… a photocatalytic, aryl radical mediated chloro-arylation reaction of alkenes. The goal was to obtain alkyl chlorides with high structural diversity from readily available alkenes and diaryliodonium salts. The developed transformation benefits from a high degree of modularity through the …
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Part I. Large scale procedure for the α-arylation of esters catalyzed by the pd(i) dimer [p(tbu)3]pd(μ-br)]2. Part II. Palladium-catalyzed γ-arylation of α,β-unsaturated esters
… report the development of a procedure for the α-arylation of esters on 42 mmol scale which did not require use of a glovebox. The coupling of 3-bromoanisole and methyl isobutyrate catalyzed by 0.075 % [(P(tBu)3Pd(μ-Br)]2 occurred in 72% yield. The reaction was performed with commercially …
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I: Catalytic Direct C-H Arylation of Pyrazoles. II: Toward Modulation of Neuroplasticity with Small Molecules
… intermolecular palladium-catalyzed direct C-H arylation of N-substituted pyrazole compounds. The scope of the reaction and the ability to sequentially and selectively arylate specific positions on the azole core to rapidly access highly substituted pyrazoles will be discussed. Part II of this …
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Applications of Hypervalent Iodine Reagents: From Enantioselective Copper-Catalysed Arylation-Semipinacol Cascade to Methionine Functionalisation for Peptide Macrocyclisation
… the thesis, diaryliodonium salts are employed as arylation reagents for the enantioselective copper-catalysed arylative semipinacol rearrangement (SPR) of various tertiary allylic alcohols. This cascade reaction is a rare example of asymmetrically activating SPR using carbon electrophiles. …
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Copper-catalyzed arylation of 1,2-amino alcohols. Synthesis of N-terminal, peptide helix initiators, and characterization of highly helical, capped polyalanine peptides
I. An improved Ullmann reaction for N- or O-arylation of 1,2-aminoalcohols with aryl iodides is described. The procedures enjoy several advantages over traditional methods: a substoichiometric amount of copper catalyst is employed, the reactions take place in low boiling and non-toxic solvents such …
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I. Multicatalysis: Development of a BiOTf₃-catalyzed Nucleophilic Addition/Hydrofunctionalization Reaction in the Synthesis of Complex Heterocycles; . . .
… most efficient and general catalysts for the C-H arylation of arenes and heteroarenes with haloarene donors. Despite the importance of this class of catalytic reactions, the mechanistic understanding is limited by the lack of direct experimental evidence, especially in the context of Lewis basic …
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New lithiation methodologies to 2-substituted nitrogen heterocycles
… for lithiation-trapping and lithiation-arylation of N-Boc heterocycles in the position α to nitrogen as well as in situ infra-red spectroscopic monitoring of lithiation reactions and the application of lithiation-arylation in total synthesis. Chapter 2 details the use of in situ …
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The development and synthetic applications of Ti- and Pd-catalyzed processes
… ee. Chapter 2. A Method for the Pd-Catalyzed y-Arylation of Ketones and its Application to a One-Pot Synthesis of Tricyclic Indolines The Pd-catalyzed ca-arylation of enolates is a rapidly growing area of chemistry due its usefulness in constructing key C-C bonds. After thorough optimization, we …
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Palladium catalyzed carbon-carbon bond formation at carbon-hydrogen bonds
… subsequent removal of activating agents. Direct arylation reactions are attractive alternatives to traditional cross-coupling methods, as one of the pre-activated partners is replaced with a simple arene. The organometallic coupling partner is typically replaced as it is the most difficult to …
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I. Anhydrous Suzuki-Miyaura cross-coupling of boronic esters enabled by potassium trimethylsilanolate II. investigations into the atropselective n-arylation of benzimidazoles utilizing the Chan-Evans-Lam coupling
Submission published under a 24 month embargo labeled 'Closed Access', the embargo will last until 2025-08-01
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COMPLEXES OF GROUP 10 METALS WITH NON-CLASSICAL AND THIOETHER-FUNCTIONALIZED N-HETEROCYCLIC CARBENE LIGANDS
… NHCs and their catalytic activities in direct arylation reactions are presented. The third part is focused on indazolin-3-ylidene ligands, their coordination chemistry with palladium(II), and catalytic applications for the direct arylation of 1-methylpyrrole, Sonogashira cross-couplings, and …
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