A5061926373- Asymmetric Synthesis and Catalysis
- X-ray Diffraction in Crystallography
- Crystallization and Solubility Studies
- Synthetic Organic Chemistry Methods
- Oxidative Organic Chemistry Reactions
- Chemical synthesis and alkaloids
- Chemical Synthesis and Analysis
- Analytical Chemistry and Chromatography
- Synthesis and Biological Activity
- Chemical Synthesis and Reactions
- Synthesis of Organic Compounds
- Insect and Pesticide Research
- Marine Sponges and Natural Products
- Marine Toxins and Detection Methods
- Cholinesterase and Neurodegenerative Diseases
- Synthesis and Reactivity of Heterocycles
- Inorganic and Organometallic Chemistry
- Nicotinic Acetylcholine Receptors Study
- Molecular spectroscopy and chirality
- Chemical Reaction Mechanisms
- Advanced biosensing and bioanalysis techniques
- Organic Chemistry Cycloaddition Reactions
- Quinazolinone synthesis and applications
- Asymmetric Hydrogenation and Catalysis
- Cancer therapeutics and mechanisms
Manchester Metropolitan University
2016-2025
Ospedale SS. Annunziata
2024
Universitatea de Medicină, Farmacie, Științe și Tehnologie „George Emil Palade” din Târgu Mureș
2024
Roosevelt University
2024
University of Auckland
2000-2013
University of Reading
1999-2000
The expanding "toolbox" of biocatalysts opens new opportunities to redesign synthetic strategies target molecules by incorporating a key enzymatic step into the synthesis. Herein, we describe general biocatalytic approach for enantioselective preparation 2,6-disubstituted piperidines starting from easily accessible pro-chiral ketoenones. strategy represents disconnection, which relies on an ω-TA-mediated aza-Michael reaction. Significantly, show that reversible process can power shuttling...
Biocatalysis is now a well-established branch of catalysis and the growing toolbox natural, evolved designer enzymes enabling chemistry previously deemed inaccessible. However, most enzyme methodologies have been developed for functional group interconversions, such as conversion ketone to an amine or alcohol, do not result in generation significant 3D molecular complexity. The application enzyme-triggered reaction cascade has potential transform simple substrates into complex sp3-rich...
Biocatalysis is now a well‐established branch of catalysis and the growing toolbox natural, evolved designer enzymes enabling chemistry previously deemed inaccessible. However, most enzyme methodologies have been developed for functional group interconversions, such as conversion ketone to an amine or alcohol, do not result in generation significant 3D molecular complexity. The application enzyme‐triggered reaction cascade has potential transform simple substrates into complex sp3‐rich...
Nucleophilic addition of Grignard reagents and organolithium species to a 3-silyloxy-3,4,5,6-tetrahydropyridine N-oxide provides trans-2,3-disubstituted N-hydroxypiperidines exclusively. The application this methodology the preparation diversity useful trans-2-substituted-3-hydroxypiperidines, concise synthesis (+)-swainsonine, an enantiopure 1-substituted quinolizidine utility in target-directed is reported.
Monomeric C-reactive protein (mCRP) has recently been implicated in the abnormal vascular activation associated with development of atherosclerosis, but it may act more specifically through mechanisms perpetuating damaged vessel inflammation and subsequent aggregation internalization resident macrophages. Whilst direct effects mCRP on endothelial cells have characterized, interaction blood monocytes has, to our knowledge, not fully defined. Here we showed that caused a strong both U937 cell...
Objectives: In this study, we examined the possibility of using targeted antibodies and potential small molecular therapeutics (acetylcholine, nicotine tacrine) to block pro-inflammatory adhesion-related properties mCRP. Methods: We used three established models (platelet aggregation assay, endothelial leucocyte binding assay monocyte inflammation via ELISA Western blotting) assess these therapeutics. Results: The results study showed that induced (raised TNF-α) by mCRP was significantly...
An ω-transaminase-triggered intramolecular aza-Michael reaction has been employed for the preparation of cyclic β-enaminones in good yield and excellent enantio- diastereoselectivity, starting from easily accessible prochiral ketoynones commercially available enzymes. The powerful thermodynamic driving force associated with spontaneous effectively displaces transaminase equilibrium towards product formation, using only two equivalents isopropylamine. To demonstrate potential this...
An efficient and flexible synthetic approach to the core structures of pinnaic acid halichlorine is described using spirocyclic nitrone 4 as a key intermediate. 1,3-Dipolar cycloaddition with dipolarophile 8 provides access azaspirocyclic 5 while spiroquinolizidine 6 has been synthesised viacycloaddition 29. Nitrone accessed by oxidative ring opening isoxazolidine 9. The utility this strategy in synthesis C5 substituted analogues also demonstrated.
Introduction The neurovascular unit (NVU), comprising vascular and glial cells along with neurons, is vital for maintaining the blood-brain barrier (BBB) cerebral homeostasis. Dysfunction of NVU implicated in key neurodegenerative disorders such as Alzheimer's disease (AD). Monomeric C-reactive protein (mCRP), dissociated form native, pentameric (pCRP), associated enhanced pro-inflammatory responses system, leading to increased permeability potential disruption. Methods This study utilized...
Abstract An alcohol dehydrogenase‐mediated asymmetric reduction and subsequent intramolecular oxa‐Michael reaction has been developed for the preparation of tetrahydropyrans (or oxanes) tetrahydrofurans, in excellent conversion, yield high enantiomeric diastereomeric excess. To highlight utility methodology, we report synthesis an analogue fungal antioxidant brocaketone A. Also described is (–)‐( R , )‐enantiomer natural product, (+)‐( S,S )‐( cis ‐6‐methyltetrahydropyran‐2‐yl)acetic acid.
Organocopper reagents are amongst the most important C-C bond forming tools available to organic chemists. Recent interest in these has focused on further developing preparative methods, exploring reactivity of functionalized cuprates and stereoselective transformations. This highlight briefly reviews advances made each areas over last five years Keywords: stereoselectivity, cross-coupling, aminoalkylcuprate, carbocupration,
The cyclisation of 3-pyridyl radicals and (2-pyridyl)methyl radicals, generated from (pyridyl)cyclohexenols 5 to 8, has been examined as part a model study directed towards the synthesis huperzine A. radical, 3-bromopyridine 5, undergoes 5-exo-trig give hexahydroindenopyridine 10.Related pyridine-fused tricycle 12 is formed by cyclization radical derived selenide 7b, while selenides 8b 19 undergo 6-exo-trig bicyclo[3.3.1]nonanecore
A concise synthesis of two novel chromeno[3,4-b]pyridin-9-ones (as their ethylene ketals) has been achieved using, as a key step, the reaction between mixed cuprate derived from 6-methoxy-2-methyl-3-lithiopyridine and 4-tert-butyldimethylsiloxycyclohex-2-enone.
The preparation of chiral pool-derived nitrone 3 and its use in the protecting-group free, stereoselective synthesis a range 1,3-disubstituted tetrahydroisoquinolines is described. Grignard reagent additions to yielded trans-1,3-disubstituted N-hydroxytetrahydroisoquinolines 6 with good levels selectivity, while 1,3-dipolar cycloadditions this provided access 3-(2-hydroxyalkyl)isoquinolines 12 as single diastereomers.
The nucleophilic addition of allylstannanes to oxycarbenium ions generated from phthalide acetate has been studied. optimum conditions involve the use trimethylsilyl trifluoromethanesulfonate in dichloromethane at -78 °C. Hydroboration allylated products followed by oxidative cyclization provides an efficient synthesis arylspiroketals which are closely related papulacandins.