A5050549214- Synthesis and Catalytic Reactions
- Tryptophan and brain disorders
- Catalytic C–H Functionalization Methods
- Asymmetric Synthesis and Catalysis
- X-ray Diffraction in Crystallography
- Oxidative Organic Chemistry Reactions
- Crystallization and Solubility Studies
- Crystallography and molecular interactions
- Fluorine in Organic Chemistry
- Synthetic Organic Chemistry Methods
- Genomics and Rare Diseases
- Criminal Justice and Corrections Analysis
- Genetics and Neurodevelopmental Disorders
- Organic Chemistry Cycloaddition Reactions
- Anesthesia and Sedative Agents
- Pharmacological Receptor Mechanisms and Effects
- Asymmetric Hydrogenation and Catalysis
- Receptor Mechanisms and Signaling
- Signaling Pathways in Disease
- Synthesis and Biological Evaluation
- Analytical Methods in Pharmaceuticals
- Glycogen Storage Diseases and Myoclonus
- Cyclopropane Reaction Mechanisms
- Crime Patterns and Interventions
- Cancer Treatment and Pharmacology
Cerevel Therapeutics (United States)
2024
University Health Network
2021-2022
Krembil Research Institute
2021-2022
University of Virginia
2016-2020
San Jose State University
2017
McGill University
2016
MacroGenics (United States)
2005
Microgen (United States)
2005
Dioxiranes are among the most selective and useful reagents for C(sp3)–H hydroxylation, but development of a general dioxirane-mediated catalytic method has been an elusive goal. A trifluoromethyl ketone catalyst in combination with Oxone is shown to enable first hydroxylations that approximate reactivity selectivity isolated dioxiranes. The mild reaction conditions allow 3° hydroxylation 2° oxidation tolerant acid-sensitive functionality electron-neutral arenes.
Formal [5 + 1] cycloadditions between aryl-substituted vinylcyclopropanes and nitrenoid precursors are reported. The method, which employs Rh2(esp)2 as a catalyst, leads to the highly regioselective formation of substituted tetrahydropyridines. Preliminary mechanistic studies support stepwise, polar mechanism enabled by previously observed Lewis acidity Rh-nitrenoids. Overall, this work expands application nitrene-transfer cycloaddition, relatively underexplored approach heterocycle...
Olefin aziridination via organocatalytic nitrene transfer offers potential complementarity to metal-catalyzed methods; however there is a lack of reports such reactions in the literature. Herein reported method that employs an iminium salt catalyze styrenes by [ N-( p-toluenesulfonyl)imino]phenyliodinane (PhINTs). These are hypothesized proceed diaziridinium as active oxidant. In addition outlining scope and limitations method, evidence for polar, stepwise mechanism presented, which provides...
Highly unusual properties of acene-based quinones 1A and 1T are reported. They undergo an unexpected combination Michael carbonyl additions aryllithium leading to new triarylated benzoperylenes 3A 3T. Uncharacteristically for quinones, display vibronically split absorption bands small Stokes shifts. The absorption/emission spectra the highly emissive almost indistinguishable from those aromatized 3A. Additional benzene rings cause a counterintuitive blue shift aromatic derivatives (2T/3T),...
Indoleamine 2,3-dioxygenase 1 (IDO1) is a promising therapeutic target in cancer immunotherapy and neurological disease. Thus, searching for highly active inhibitors use human cancers now focus of widespread research development efforts. In this study, we report the structure-based design 2-(5-imidazolyl)indole derivatives, series novel IDO1 which have been designed synthesized based on our previous study using N1-substituted 5-indoleimidazoles. Among these, identified one with strong...
Predictably site-selective catalytic methods for intermolecular C(sp3)–H hydroxylation and amination hold great promise the synthesis late-stage modification of complex molecules. Transition-metal catalysis has been most common approach early investigations this type reaction. In comparison, there are far fewer reports organocatalytic direct oxygen or nitrogen insertion into C–H bonds. Herein, we provide an overview efforts in area, with particular emphasis on our own recent development...
Pulmonary interstitial glycogenosis is an lung disease of childhood that has been increasingly reported over the past decade. Here, we present a case pulmonary associated with trisomy 21, arterial hypertension, and congenital heart in 34 week premature infant.
The design of potent indoleamine 2,3-dioxygenase 1 (IDO1) enzyme inhibitors targeting immunopathic neuroinflammation has emerged as an area interest for the treatment Alzheimer's disease (AD); additionally, recent findings on clinical benefits antibodies preventing β-amyloid (Aβ) aggregation have renewed efforts to discover small molecule anti-aggregants proteopathic protein misfolding. Exploiting endogenous tryptophan-like scaffold, we describe and synthesis small-molecule both processes,...
s: Ninth International Congress of Therapeutic Drug Monitoring and Clinical Toxicology: Louisville, Kentucky April 23-28, 2005
Key words isoindolinones - isoxazoles cascade reaction cyclization