A5088881106- Crystallization and Solubility Studies
- X-ray Diffraction in Crystallography
- Catalytic C–H Functionalization Methods
- Synthesis and Catalytic Reactions
- Chemical Synthesis and Analysis
- Catalytic Cross-Coupling Reactions
- Click Chemistry and Applications
- Cyclopropane Reaction Mechanisms
- Sulfur-Based Synthesis Techniques
- Synthesis and biological activity
- Asymmetric Synthesis and Catalysis
- Fluorine in Organic Chemistry
- Analytical Chemistry and Chromatography
- Neuroscience and Neuropharmacology Research
- Inflammatory mediators and NSAID effects
- Synthetic Organic Chemistry Methods
- Crystallography and molecular interactions
- Computational Drug Discovery Methods
- Synthesis and Biological Evaluation
- Chemical synthesis and alkaloids
- Alzheimer's disease research and treatments
- Microtubule and mitosis dynamics
- Chemical Synthesis and Reactions
- Enzyme Catalysis and Immobilization
University of Pennsylvania
2016-2023
Laboratoire COBRA
2011-2018
Centre National de la Recherche Scientifique
2011-2018
Université de Rouen Normandie
2011-2018
Normandie Université
2018
Institut National des Sciences Appliquées Rouen Normandie
2012-2018
Différenciation et Communication Neuronale et Neuroendocrine
2018
ESPCI Paris
2017
Université Paris Sciences et Lettres
2017
Génétique Moléculaire Génomique Microbiologie
2012-2017
The replacement of a carboxylic acid with surrogate structure, or (bio)-isostere, is classical strategy in medicinal chemistry. general underlying principle that by maintaining the features critical for biological activity, but appropriately modifying physicochemical properties, improved analogs may result. In this context, systematic assessment properties isosteres would be desirable to enable more informed decisions potential replacements used analog design. Herein we report...
Catalytic direct (hetero)arylation of (hetero)arenes is an attractive alternative to traditional Kumada, Stille, Negishi and Suzuki–Miyaura cross-coupling reactions, notably as it avoids the prior preparation isolation (hetero)arylmetals. Developments this methodology in oxazole series are reviewed article. Methodologies, selectivity, mechanism future aspects presented.
Neurodegenerative disorders referred to as tauopathies, which includes Alzheimer's disease (AD), are characterized by insoluble deposits of the tau protein within neuron cell bodies and dendritic processes in brain. Tau is normally associated with microtubules (MTs) axons, where it provides MT stabilization may modulate axonal transport. However, becomes hyperphosphorylated dissociates from MTs evidence reduced stability defective This has led hypothesis that MT-stabilizing drugs have...
Abstract Both base‐assisted non‐concerted metallation–deprotonation (nCMD) and concerted (CMD) have been identified as two potent operating mechanisms in palladium‐catalysed direct CH coupling of oxazole thiazole‐4‐carboxylate esters with halides through base‐ solvent‐effect experiments. Novel C2‐ C5‐selective CMD arylation procedures oxazole‐ series were then designed by controlling the balance between electronic steric factors. Notably, charge interactions palladium catalyst substrate a...
The oxetane ring serves as an isostere of the carbonyl moiety, suggesting that oxetan-3-ol may be considered a potential surrogate carboxylic acid functional group. To investigate this structural unit, well thietan-3-ol and corresponding sulfoxide sulfone derivatives, bioisosteres, set model compounds has been designed, synthesized, evaluated for physicochemical properties. Similar derivatives cyclooxygenase inhibitor, ibuprofen, were also synthesized inhibition eicosanoid biosynthesis in...
A Regel-type transition-metal-free direct C-2 aroylation of (benzo)oxazoles, (benzo)thiazoles and 1,3,4-oxadiazoles with acid chlorides catalyzed by <i>N</i>,<i>N</i>-dimethyl-4-aminopyridine (DMAP) is described. This methodology effective several aroyl heteroaroyl affording the corresponding 2-ketoazoles in moderate to excellent yields.
Hydrogen bonding is a key molecular interaction in biological processes, drug delivery, and catalysis. This report describes high throughput UV-Vis spectroscopic method to measure hydrogen capacity using pyrazinone sensor. colormetric sensor reversibly binds bond donor, resulting blue shift as additional equivalents of donor are added. Titration with excess used determine the binding coefficient, ln(K
Herein, palladium-catalyzed Miyaura borylation of 4-bromo-2,4'-bithiazoles followed by Suzuki-Miyaura cross-coupling reaction (named the MBSC process) with (hetero)aryl- and alkenyl halides is reported. This methodology offers rapid access to various 2',4-disubstituted 2,4'-bithiazole features including naturally-occurring 4-alkenylated 4-pyridinylated 2,4'-bithiazoles. To prove its application, a concise approach for synthesis heterocyclic cluster thiopeptide d-series antibiotic GE2270...
A straightforward enantiomerically pure synthesis of the heterocyclic core D-series GE2270 is reported. The synthetic strategy combines Hantzsch thiazole's building condensation with a cross-coupling reaction including direct C-H hetarylation to build and connect step-by-step thiazolyl moieties 5-bromopicolinate as readily available starting material.
2‐(1 H ‐1,2,4‐Triazol‐1‐yl)ethanols have received significant interest in agricultural and medicinal chemistry owing to their herbicidal antifungal activities. To develop a versatile method access these substituted triazoles, we explored the generation of (1 ‐1,2,4‐triazol‐1‐yl)methyl carbanion its condensation with carbonyl compounds. By judicious choice suitable anion precursor (tributylstannyl group) or stabilizing group (phenylsulfanyl phenylsulfinyl group), wide range aldehydes ketones...
Abstract The general and efficient method allows the synthesis of a wide range 2‐ketoazoles via metal free reaction oxazoles thiazoles with acid chlorides.