A5023948531- Catalytic C–H Functionalization Methods
- Radical Photochemical Reactions
- Crystallization and Solubility Studies
- X-ray Diffraction in Crystallography
- CO2 Reduction Techniques and Catalysts
- Receptor Mechanisms and Signaling
- Catalytic Cross-Coupling Reactions
- Sulfur-Based Synthesis Techniques
- Speech Recognition and Synthesis
- Cystic Fibrosis Research Advances
- Synthesis and Catalytic Reactions
- Axial and Atropisomeric Chirality Synthesis
- Organoboron and organosilicon chemistry
- Pharmacogenetics and Drug Metabolism
- Chemical synthesis and alkaloids
- Asymmetric Hydrogenation and Catalysis
- Ferrocene Chemistry and Applications
- Alkaloids: synthesis and pharmacology
- Respiratory viral infections research
- Synthesis and Biological Evaluation
- Renin-Angiotensin System Studies
- Neonatal Respiratory Health Research
- Adenosine and Purinergic Signaling
- Organic Chemistry Cycloaddition Reactions
- Taxation and Legal Issues
Uppsala University
2022-2024
Leo Pharma (Denmark)
2022-2024
Science for Life Laboratory
2022-2024
Leo Pharma (Australia)
2022
A useful protocol for achieving decarboxylative cross-coupling (DCC) of redox-active esters (RAE, isolated or generated in situ) and halo(hetero)arenes is reported. This pragmatically focused study employs a unique Ag-Ni electrocatalytic platform to overcome numerous limitations that have plagued this strategically powerful transformation. In its optimized form, coupling partners can be combined surprisingly simple way: open the air, using technical-grade solvents, an inexpensive ligand Ni...
Early diagnosis and treatment is considered important to prevent lung damage in primary ciliary dyskinesia (PCD).Few studies have addressed long-term evolution of function after PCD diagnosis. We investigated whether was dependent on age or level at diagnosis.An observational, single-center, cross-sectional, three-decade longitudinal study FEV(1) FVC related until current performed. Linear regression used describe the relation between first measured values across cohort. Courses according...
Abstract There is a pressing need, particularly in the field of drug discovery, for general methods that will enable direct coupling tertiary alkyl fragments to (hetero)aryl halides. Herein uniquely powerful and simple set conditions achieving this transformation with unparalleled generality chemoselectivity disclosed. This new protocol placed context other recently reported methods, applied simplify routes known bioactive building blocks molecules, scaled up both batch flow. The role...
A concise and enantioselective total synthesis of the Veratrum alkaloid cyclopamine is disclosed. This highly convergent with a 16-step longest linear sequence (LLS) was enabled by de novo trans-6,5-heterobicycle via strain-inducing halocyclization process, key Tsuji–Trost cyclization to construct fully substituted, spirocyclic THF motif exquisite diastereocontrol, late-stage ring-closing metathesis (RCM) reaction forge central tetrasubstituted olefin.
Abstract There is a pressing need, particularly in the field of drug discovery, for general methods that will enable direct coupling tertiary alkyl fragments to (hetero)aryl halides. Herein uniquely powerful and simple set conditions achieving this transformation with unparalleled generality chemoselectivity disclosed. This new protocol placed context other recently reported methods, applied simplify routes known bioactive building blocks molecules, scaled up both batch flow. The role...
There is an urgent need, particularly in the field of drug discovery, for general methods that will enable direct coupling tertiary alkyl fragments to (hetero)aryl halides. This early disclosure serves this purpose by informing community a uniquely powerful and simple set conditions achieving transformation with unparalleled generality chemoselectivity.
Two series of N-(heteroaryl)thiophene sulfonamides, encompassing either a methylene imidazole group or tert-butylimidazolylacetyl in the meta position benzene ring, have been synthesized. An AT
Ligands comprising a benzimidazole rather than the imidazole ring that is common in AT2R ligands e.g. agonist C21, can provide both high affinity and receptor selectivity. In particular, compounds encompassing benzimidazoles, substituted 2-position with small bulky groups such as an isopropyl (Ki = 4.0 nM) or tert-butyl 5.3 alternatively thiazole heterocycle 5.1 demonstrate An n-butyl chain, found AT1R selective sartans, makes ligand less selective. The isobutyl group on biaryl scaffold...
The polar retrosynthetic analysis has been widely employed in the field of organic synthesis and forms basis undergraduate curriculum. Although most reactions rely on this rubric to guide their strategic application, implementation often requires a long list ancillary considerations mitigate chemoselectivity oxidation state issues involving protecting groups precise reaction choreography. Here we demonstrate complete departure from norm by use radical based Ni/Ag-electrocatalytic cross...
A useful protocol for achieving decarboxylative cross coupling (DCC) of redox-active esters (RAE, isolated or generated in situ) and halo(hetero)arenes is reported. This pragmatically focused study employs a unique Ag-Ni electrocatalytic platform to overcome numerous limitations that have plagued this strategically powerful transformation. In its optimized form partners can be combined surprisingly simple way: open the air, technical grade solvents, an inexpensive ligand Ni source,...
There is a pressing need, particularly in the field of drug discovery, for general methods that will enable direct coupling tertiary alkyl frag-ments to (hetero)aryl halides. Herein uniquely powerful and simple set conditions achieving this transformation with unparalleled generality chemoselectivity disclosed. This new protocol placed context other recently reported methods, applied simplify routes known bioactive building blocks molecules, scaled up both batch flow. The role pyridine...
The syntheses and the AT1R AT2R binding data of a series new small molecule ligands are reported. These comprise phenylthiazole scaffold rather than biphenyl or phenylthiophene scaffolds found in essentially all previously described originating from nonselective AT1R/AT2R ligand L-162,313 selective agonist C21, latter now Phase II/III clinical trials. A that is present C21 antagonist C38 had deleterious effect on affinity to AT2R. Nevertheless, significant improvement could be accomplished...
Two series of N-(heteroaryl)thiophene sulfonamides, encompassing either a methylene imidazole group or tert-butylimidazolylacetyl in the meta position benzene ring, have been synthesized. An AT2R selective ligand with Ki 42 nM was identified first and second series, six ligands significantly improved binding affinities values < 5 were discovered. The modes to explored by docking calculations combined molecular dynamics simulations. Although some high affinity exhibited fair stability human...