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Showing 1 to 20 of 31 for “"Aziridine"”.
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Synthesis and Evaluation of Aziridine Analogs of Presqualene Diphosphate as Squalene Synthase Inhibitors
The enhanced inhibitory activities of these novel aziridine diphosphate and methanediphosphonates towards squalene synthase compared to the analogous acyclic azabifarnesyl diphosphate may indicate a bridged non-classical, protonated cyclopropane intermediate in the formation of presqualene …
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Convergent Site-Selective Carbohydrate-Peptide Ligations With Dehydroalanine and Aziridine -2 -Carboxylic Acid-Containing Peptides
… through the incorporation of dehydroalanine and aziridine-2-carboxylic acid residues into peptides and subsequent conjugation of the resulting peptide electrophiles with various thiols. Oligosaccharides incorporating a suitable anomeric thio-functionality were prepared via dehydrative …
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Electrophilic Affinity Labels and Fluorescent Conjugates for the Estrogen Receptor (Norhexestrol, Aziridine, Hexestrol, Fluorescein, Alkylator)
We prepared several aziridine derivatives of the potent, non-steroidal estrogen hexestrol ((3R*,4S*)-3,4-bis(4-hydroxyphenyl)hexane)) in search of an estrogen agonist that achieves selective, efficient labeling of the estrogen receptor. The electrophilic agent, aziridine, was positioned at a side …
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Synthesis and evaluation of aziridine and symmetry-based epoxide affinity labels for HIV-1 protease
… of three symmetry-based epoxides and an aziridine analog of 1,2-epoxy-3-(p-nitrophenoxy)propane (EPNP) are reported. Assay procedures were developed to allow testing for both reversible and irreversible inhibition of HIV-1 protease, based on an internally-quenched fluorogenic substrate. …
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Chelating compounds as potential flash rust inhibitors and melamine & aziridine cure of acrylic colloidal unimolecular polymers (CUPs)
… coating with either a melamine (bake) or an aziridine (ambient cure) and then cured. The melamine system was solvent free, a near zero VOC and the aziridine system was very low to near zero VOC. The coatings were evaluated for their MEK resistance, adhesion, hardness, gloss, flexibility, wet …
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Ring-Opening of Aziridine -2 -Carboxamides by Carbohydrate C1-O Nucleophiles. Stereoselective Preparation of O-Linked Glycopeptides
… carbohydrate C1-O nucleophilic ring-opening of aziridine-2-carboxamides to access the target O-linked glycopeptides. The synthesis of the alpha-GalNAc-Ser class of glycopeptides is emphasized and either the alpha- or beta-glycoside can be accessed by judicious selection of solvent and metal …
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Studies towards the Organocatalytic ‘Dialled In’ Synthesis of Chiral, Non-Racemic Aziridines, and Amino Acids, Containing Multiple Isotopic Labels
… highly cis-selective synthesis of N-aryl 3-aryl-aziridine-2-carboxylates as racemates in yields of up to 80 %. This methodology has been extended by the use of a highly acidic C2 symmetric 3,3’- anthracenyl functionalised BINOL triflylphosphoramide organocatalyst, which allows for the formation …
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Potential Antiestrogen-Based Cytotoxic Agents and an Affinity Label for the Estrogen Receptor
… using an affinity labeling compound, tamoxifen aziridine (TA).
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Analysis of Estrogen and Antiestrogen Receptor Complexes
… affinity labeling estrogen, ketononestrol aziridine (KNA).
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Organocatalytic synthesis of chiral non-racemic aziridines, labelled with 2H, 15N, 13C stable isotopes
Aziridines are ‘keystone’ synthetic building blocks - relatively reactive, three-membered heterocycles with the potential for generating ‘secondary’ high value entities such as α- or β-amino acids via ring-opening reactions. Within this thesis, a one-pot asymmetric organocatalytic methodology is …
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The Asymmetric Total Synthesis of Cephalotaxine
… rearrangement of 1-vinyl-2-aryl-aziridines, has been developed and applied to the synthesis of the Cephalotaxus alkaloids. The synthetic approach begins with D-ribose and utilizes the [3,3] sigmatropic rearrangement of a highly functionalized 1-vinyl-2-aryl aziridine and a …
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Nickel precatalysts as enabling tools for catalytic coupling reactions
… cross-coupling of aliphatic N-tosylaziridines with aliphatic organozinc reagents is described. The reaction protocol displays complete regioselectivity for reaction at the less hindered C-N bond, and the products are furnished in good to excellent yield for a broad selection of …
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New Methods For The Synthesis Of Oxygen And Nitrogen Containing Heterocycles
… The copper catalyzed ring expansion of vinylaziridines produces nitrogen containing heterocycles commonly found in pharmaceuticals and natural products. This reaction is described from its initial discovery, through optimization, to application. Many substitution patterns and functional …
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Two enantiodivergent syntheses of balanol and the chemoenzymatic synthesis of oseltamivir
… each proceeding through a different vinyl aziridine derived from bromobenzene and ethyl benzoate.
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Asymmetric synthesis of benzylic and heterobenzylic amines
… carbonate. Asymmetric synthesis of 2-(2-pyridyl)aziridines from chiral 2-pyridineimines bearing a stereogenic center at the nitrogen atom was development. The envisioned route involves the addition of chloromethyllithium to the imine derived from 2-pyridinealdehyde and (S)-valinol, protected as …
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Chemistry with chiral lithium amides: enantiotopic group and face-selective reactions
… esters of tropinone and the enantioselective aziridine formation from nortropinone is first reported. This opened two new paths to develop tropinone enolate chemistry. One is indirect α-alkylation of tropinone, another is the nucleophilic attack from α-C enolate to the nitrogen atom. Seven …
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Asymmetric Dihydroxylation and Aziridination of Allenes and Related Chemistry
… and allene substitution are also discussed. Aziridines were formed by copper-catalyzed intramolecular nitrene addition to alkenes. The carbamate group was used as the tether between the alkene and the nitrene. Subsequent nucleophilic attack of the aziridine was accomplished using RSH, R2NH, …
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Synthesis of Cytotoxic Antiestrogens and Control Compounds (Nafoxidine)
… receptor during binding of the ligand. The aziridine derivative of desmethylnafoxidine formed a covalent attachment in the estrogen binding site with 80% of the estrogen receptor within 1 hour when it was present in a 10-fold excess.
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Novel copper-catalysed coupling reactions of diphenylmethane
… a soft nucleophilic attack on N-α-phenylethyl aziridine. Upon carrying out this reaction, no desired product was formed, even with the addition of a Lewis acid. A review of the NMR spectra of the crude reaction mixture indicated that significant amounts of both diphenylpentane and tetraphenyl …
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