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Showing 1 to 20 of 48 for “"Amidation"”.
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Synthesis and reactivities of titanocene-oxo complexes and rhodium-catalyzed oxidative amidation
… thesis focuses on rhodium-catalyzed oxidative amidation reactions. Amides are an important functional group commonly found in natural products and pharmaceuticals, and are traditionally prepared via amidation reactions involving stoichiometric activation of carboxylic acids, either in the form …
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Development of a copper-catalyzed amidation-base-promoted cyclization sequence for the synthesis of 2-aryl- and 2-vinyl1-4 quinolones
… that utilizes a copper-catalyzed amidation of ortho-halophenones followed by a base-promoted Camps cyclization of the resulting N-(2-keto-aryl)amides is described. With Cul, a diamine ligand, and base as the catalyst system, the amidation reactions proceed in good yields for a …
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ENZYME ENGINEERING AND GREEN SYNTHESIS OF N-ACYL GLYCINE BIOSURFACTANTS FROM RENEWABLE RAW MATERIALS
… Herein, we report a novel concept for enzymatic amidation in an aqueous system via glycerol activation of fatty acids and their subsequent aminolysis with glycine to synthesize N-acyl glycines. We then engineer an enzyme (proRML) by reshaping its catalytic pocket to enhance its aminolysis …
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Ruthenium Hydride Catalyzed Silylvinylation of Alkynes
… in three steps utilizing a palladium catalyzed amidation-cyclization strategy. N-Aryl substrates were synthesized using copper catalyzed amidation of 3-amino-N-Boc-4-chloropyridine. Complementary protocols for the selective chlorination of imidazo[4,5-c]pyridines at C2 and C7 positions were also …
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Syntheses of novel acyclic amino-amido ligands
… from appropriately C-functionalized malonates by amidation with N,N-dimethylethylenediamine (62) followed by reduction of the respective nitro (64) and cyano (63) groups is described. The synthesis of N,N'-bis[2-(N'',N''-dimethylamino)ethyl]iminodiacetamide (73) from diethyl N-benzyliminodiacetate …
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Heterologous production of recombinant peptidylglycine α-amidating monooxygenase for the production of biosimilar α-amidated peptides
… DNA technologies but require C-terminal amidation for maximum biological activity. Peptidylglycine α-amidating monooxygenase (PAM) is the only enzyme that catalyses the C-terminal amidation of peptides in vivo through its two catalytic cores, peptidylglycine α-hydroxylating monooxygenase …
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The development of new synthetic strategies and methodologies for complex alkaloid total synthesis : a concise synthesis of (+)-chimonanthine, (+)-WIN 64821, (-)-ditryptophenaline and related alkaloids
… Hydrogen Bonds. Studies and Application in the Amidation of Unactivated Esters. A single-step and catalytic amidation of unactivated esters with amino alcohols is described. Treatment of equimolar quantities of amino alcohols and unactivated esters with N,Nbismestiylimidazolylidene (5 mol%) …
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Neuropeptidomics: MS-base peptide identification and quantitation study
… and post-translational processing through alpha-amidation has been studied with different MS-based approaches such as matrix-assisted laser desorption/ionization time-of-flight (MALDI-TOF) MS and electrospray ionization ion-trap (ESI-IT) MS. DIMM, a transcription factor in Drosophila, appears …
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Development of Pd Catalyzed Amidations & Applications to the Synthesis of Heterocycles
… core.</p> <p>Chapter 5</p> <p>A copper catalyzed amidation of Boc protected 4-chloro-3-aminopyridine was accomplished to produce a number of aryl and heteroaryl 4-chloro-3-aminopyridines. These pyridines were used to synthesize regioselectively substituted imidazo[4,5-c]pyridines using a …
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The development of novel organocatalytic and transition-metal catalysed methodologies for amide bond formation
… such approach is the trifluoroethanol-catalysed amidation of unactivated ester derivatives. However, in the initial studies, the general applicability of this methodology was limited by the incompatibility of acyclic secondary amines under the reaction manifold, and additionally, stereoerosion …
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Identification and evaluation of bioactive peptides from amphibian skin and rational design of new analogues
… of cationicity, hydrophobicity and C-terminal amidation on bioactivity. Extended hydrophobic face exhibited higher haemolytic activity and anti-proliferative activity. cationicity-enhanced analogue exhibited higer antimicrobial activity without increasing haemolytic activity.finally, C-terminal …
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C(sp2)–H Functionalizations Employing 2-Aminophenyl-1H-pyrazole as a New Removable Directing Group
… copper-mediated aerobic oxidative C(sp2)–H bond amidation and sulfonamidation bearing a wide range of sulfonamides, When Cu(OAc)2 was employed as the copper source, 1,1,3,3-tetramethylguanidine (TMG) as an organic base, the reaction, optimally carried out overnight in DMSO at 80 °C in open air, …
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Palladium-catalyzed C-N cross-coupling and application to the synthesis of delayed singlet emitters for OLED development
… In Chapters 1 and 2, the palladium-catalyzed amidation and amination of five-membered heterocyclic bromides containing multiple heteroatoms are described. These methods provide efficient access to N-arylated imidazoles and pyrazoles in moderate to excellent yields. In Chapter 3, a series of …
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TEMPO-oxidized Nanocelluloses: Surface Modification and use as Additives in Cellulosic Nanocomposites
… In the first part of the work, covalent (amidation) and non-covalent (ionic complexation) coupling were compared as treatment techniques for the hydrophobization of TONc surfaces with octadecylamine (ODA). Subsequently, TONc and its covalently coupled derivative were evaluated as nanofiber …
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Chain-end functionalization and modification of polymers using modular chemical reactions
… (copper-catalyzed or copper-free) or amidation to couple synthetic polymers to other synthetic polymers, biomolecules or silica monoliths. Using this general strategy and designing these co/polymers so that they are thermoresponsive, yet bioinert and biocompatible with adjustable cloud …
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Studies of the Physical Stability of GLP-1 & Chemically Modified Forms of GLP-1
… in solution during aggregation. The influence of amidation at the C-terminus of GLP-1 on physical stability was assessed and significant differences to GLP-1 were found. The study of this relatively small modification generates a better understanding of the interdependence of net charge, …
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Synthesis and characterization of polyamidoamine dendrons
… phase grafted onto the silica gel and (2) amidation of the resulting ester moieties with alkylene diamine, the silica particles were treated with 3-aminopropyltriethoxysilane that would serve as a coupling agent. Afterwards, the cleavage of the solid-phase synthesized full generation PAMAM …
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Part 1: Lanthanum(III) Triflate-Catalyzed Cyclopropanation via Intramolecular Methylene Transfer. Part 2: Reaction Design with Aromatic Ions - Nucleophilic Acyl Substitution and Organophotoredox Catalysts
… on the rate of conversion is examined. A mild amidation protocol employing acid chloride formation is described and applied to acid-sensitive substrates and preparative peptide couplings. The final chapter discloses the development of aromatic cation photoredox catalysts. Investigations into …
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Synthesis Of A Novel Family Of Amide Derivatives Of Podocarpic Acid
… to give iodomethyl-O-methylpodocarpate. Finally amidation with various aliphatic amides using a copper catalyst yielded four amide derivatives of podocarpic acid. However, iodomethyl-O-methylpodocarpate did not react with aromatic amides. This is perhaps because of the reduction in …
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Synthesis and Application of Boronic Acid Derivatives
… °-alkylation, saponification/hydrogenation, amidation, and oxidative removal of pinacolyl group with sodium periodate. A simple amidoboronic acid was also synthesized for stability studies. This compound, synthesized in 44% overall yield, could be used as a surrogate for N-terminal peptidic …
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