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Characterization and Exploitation of Bidirectional Allosteric Coupling in Multi-Domain Tyrosine Kinases using Conformation-Selective ATP-Competitive Inhibitors
Protein kinases are a large family of enzymes that play integral roles in cell signaling networks and are thus critical for effecting appropriate cellular responses to environmental stimuli. Much of kinase biological function has been studied in terms of catalytic activity: phosphorylation of substrate proteins as part of ...
Palladium-Catalyzed Cross-Couplings of 2-Alkylaziridines and Alkenylboronic Acids
A new method to synthesize substituted homoallylic amines is reported. Homoallylic amines are important structural moieties in natural products and pharmaceutical agents. The reaction couples N-nosyl-2-alkylaziridines with alkenylboronic acids under palladium catalysis. This work examines the role of base and proton donor ...
Enantioselective Diamination of Alkenes, Hydroamination of 1,3-Dienes, and the Development of NHC Palladium Complexes
(2014-04-30)
Nitrogen containing heterocylces make up a vast majority of biologically relevant small molecules. Using transition metal catalysts to directly synthesize functionalized amine heterocycles is a valuable and efficient tool in chemical synthesis. Herein, the development of two palladium-catalyzed transformations are described; ...
Development of Palladium and Hypervalent Iodine(III) Catalyzed Alkene Difunctionalization Reactions; Hydroamination, Carboamination, Aminofluorination & Diamination
(2014-04-30)
The investigation and development of synthetic methodologies for direct alkene difunctionalization is described. The utility of these processes is demonstrated by the synthesis of a number of functionalized nitrogen-containing heterocycles, including pyrrolidines and morpholines. As these are commonly-encountered motifs in a ...
The Discovery, Development, and Mechanistic Investigations of Transition Metal-Catalyzed Organic Reactions
Organic reactions have wide spread applications in drug development, chemical biology, and materials science. However, traditional chemical techniques can be inefficient i.e., low yields and/or poor selectivity, for constructing structurally complex motifs and for selectively activating strong bonds. To address these problems, ...
Copper-Catalyzed Reactions of Organoboron Compounds
(2014-02-24)
The discovery, development, scope, and mechanistic studies of three new copper-catalyzed transformations of organoboron compounds are described herein. Specifically, Chapter 1 details the development and scope of the first general method for SN2'-selective substitution of primary allylic chlorides using aryl boronic esters ...
Gold-Catalyzed Asymmetric Synthesis of Cyclic Ethers and Copper-Catalyzed Hydrofunctionalization of Alkynes
Gold-catalyzed cyclization of enantioenriched trisubstituted allenols to form enantioenriched α-tetrasubstituted cyclic ethers has been developed. This structural motif can be found in many natural products that have useful biological properties. The cyclization reaction is compatible with multiple functional groups and can ...
Fundamental and Applied Investigations in Solid-State Polymer Mechanochemistry
The translation of mechanical force to specific chemical reactivity within polymeric materials is known as polymer mechanochemistry. While this phenomenon has long been observed in homopolymers, it has recently attracted much interest as researchers have developed systems capable of site-specific activation and defined outputs ...
From Energy Generation to Storage: The Exploration of Unusual Architectures and Functions of Conjugated Organic Molecules
The advent of conjugated polymers spurred the field of organic electronics. Since the inception of the field, many have lauded the potential benefits of organic over inorganic platforms, including their light weight, flexibility, and solution-processability, the latter of which makes them amenable to large-scale mass production. ...
Cross-Conjugated Moieties as Design Motifs for a Class of Novel Electro-Optic Chromophores
(2014-04-30)
Organic electro-optic materials are at the forefront of current photonics applications that enable high speed data transmission, micro-scale sensors, and terahertz applications. Typically linearly conjugated push-pull type chromophores are the primary molecules of choice for various second and third order non-linear optical ...