A5037436448- X-ray Diffraction in Crystallography
- Crystallization and Solubility Studies
- Radical Photochemical Reactions
- Synthesis and Catalytic Reactions
- Crystallography and molecular interactions
- Catalytic C–H Functionalization Methods
- Protein Degradation and Inhibitors
- Computational Drug Discovery Methods
- Chemical Synthesis and Analysis
- Chemistry and Chemical Engineering
- Innovative Microfluidic and Catalytic Techniques Innovation
- Melanoma and MAPK Pathways
- CO2 Reduction Techniques and Catalysts
- Pharmaceutical and Antibiotic Environmental Impacts
- Bioactive Compounds and Antitumor Agents
- Fluorine in Organic Chemistry
- Oxidative Organic Chemistry Reactions
- Click Chemistry and Applications
- Polyoxometalates: Synthesis and Applications
- Chemical Reactions and Isotopes
- Synthesis and biological activity
- Electrochemical Analysis and Applications
- Monoclonal and Polyclonal Antibodies Research
- Cytokine Signaling Pathways and Interactions
- NF-κB Signaling Pathways
Age UK
2013-2024
GlaxoSmithKline (United Kingdom)
2009-2022
North Hertfordshire College
2015-2016
New Frontier
2009
Updated methodology and scoring of the sustainability credentials a total 154 solvents, including 44 new additions.
A practical, catalytic entry to α,α,α-trisubstituted (α-tertiary) primary amines by C-H functionalisation has long been recognised as a critical gap in the synthetic toolbox. We report simple and scalable solution this problem that does not require any situ protection of amino group proceeds with 100 % atom-economy. Our strategy, which uses an organic photocatalyst combination azide ion hydrogen atom transfer (HAT) catalyst, provides direct synthesis α-tertiary amines, or their corresponding...
Reagent guides ranking commonly used reagents for 15 transformations have been developed to reduce the environmental impact of drug discovery and development. Reagents scored by a combination health, safety risk phrases, life cycle analysis (where possible) an assessment chemistry including considerations atom efficiency, stoichiometry, work-up other issues. Guides covering alkene reduction, amide formation, C–H bromination, chlorination, deoxychlorination, epoxidation, ester ether...
Abstract Out of more than 5683 clinical trials testing anti-PD1/PDL1 mAbs, on average only 20% patients achieved an objective response, leaving unmet need for who do not respond to immune checkpoint inhibitors (ICIs)(Zhao et al, 2020, Upadhyaya 2022). Independent reports in NSCLC and melanoma suggest that non responders ICI exhibit elevated levels tumor “aerobic” glycolysis (Renner 2019, Silva 2022), a phenotype associated with solid metastatic cells (Hanahan, Aerobic results accumulation...
Chiral fluorolactam derivatives bearing a fluorine atom at stereogenic centre were synthesized by combination of selective direct fluorination using gas and biochemical amidase cyclisation process.
Abstract Using High‐Throughput Experimentation (HTE), a visible light‐mediated etherification method was developed, employing the organic photocatalyst thioxanthen‐9‐one (TXO) and commercially available, air‐stable nickel source. Design of Experiments (DoE) techniques were utilized in conjunction with HTE to identify optimal reaction conditions which are mild, cost‐effective, robust therefore suitable for use an industrial setting. A diverse substrate scope prepared via parallel synthesis...
Abstract A mechanistic study on use of alternating potential (i. e. electrode polarity switching) in synthetic organic electrochemical method development using the IKA ElectraSyn 2.0 is described. Unexpected product selectivity challenges revealed that facilitated direct, rather than mediated, benzylic C−H oxidation toluene derivatives. Whilst constant irrespective direction was expected, our in‐depth analysis changes magnitude applied with periodic switching polarity. These findings...
The identification and progression of a potent selective series isoquinoline inhibitors IkappaB kinase-beta (IKK-beta) are described. Hit-generation chemistry based on IKK-beta active-site knowledge yielded weakly but tractable chemotype that was rapidly progressed into with robust enzyme cellular activity significant selectivity over IKK-alpha.
Abstract A practical, catalytic entry to α,α,α‐trisubstituted (α‐tertiary) primary amines by C−H functionalisation has long been recognised as a critical gap in the synthetic toolbox. We report simple and scalable solution this problem that does not require any situ protection of amino group proceeds with 100 % atom‐economy. Our strategy, which uses an organic photocatalyst combination azide ion hydrogen atom transfer (HAT) catalyst, provides direct synthesis α‐tertiary amines, or their...
The counter-electrode process of an organic electrochemical reaction is integral for the success and sustainability process. Unlike oxidation reactions, processes reduction reactions remain limited, especially deep reductions that apply very negative potentials. Herein, we report development a bromide-mediated silane nonaqueous in undivided cells. system found to be suitable replacing either sacrificial anodes or divided cell several reported reactions. conditions are metal-free, use...
Inhibition of Itk potentially constitutes a novel, nonsteroidal treatment for asthma and other T-cell mediated diseases. In-house kinase cross-screening resulted in the identification an aminopyrazole-based series inhibitors. Initial work on this highlighted selectivity issues with several kinases, particularly AurA AurB. A template-hopping strategy was used to identify aminobenzothiazole inhibitors, which utilized inherently more selective hinge binding motif. Crystallography modeling were...
This article describes two routes toward the synthesis of cis or trans C2,3,5,7-tetrasubstituted dihydrobenzofurans as potent and selective bromodomain extra-terminal BD2 inhibitors, followed by optimization lead molecule GSK973 to support pre-clinical efficacy safety studies. The use flow chemistry for a Claisen rearrangement, extensive fluorination step, high-yielding aminocarbonylation were key generate required 50 g material. identified new route also represents robust starting point...
A practical, catalytic entry to α,α,α‑trisubstituted (α‑tertiary) primary amines by C–H functionalisation has long been recognised as a critical gap in the synthetic toolbox. We report simple and scalable solution this problem that does not require any situ protection of amino group proceeds with 100% atom-economy. Our strategy, which uses an organic photocatalyst combination azide ion hydrogen atom transfer (HAT) catalyst, provides direct synthesis C -alkylated or γ‑lactams, including...
ADVERTISEMENT RETURN TO ISSUEPREVAddition/CorrectionNEXTORIGINAL ARTICLEThis notice is a correctionCorrection to "Multigram Synthesis of Tetrasubstituted Dihydrobenzofuran GSK973 Enabled by High-Throughput Experimentation and Claisen Rearrangement in Flow"Catherine M. Alder*Catherine AlderMore Catherine Alderhttps://orcid.org/0000-0001-7484-460X, Matthew GrayMatthew GrayMore Gray, Chelsea A. HuffChelsea HuffMore Huff, Calvin O. ManningCalvin ManningMore Manning, Alex PrestonAlex PrestonMore...