A5016669355- Asymmetric Synthesis and Catalysis
- Synthetic Organic Chemistry Methods
- Chemical Synthesis and Analysis
- Asymmetric Hydrogenation and Catalysis
- Catalytic Alkyne Reactions
- Cyclopropane Reaction Mechanisms
- Plant biochemistry and biosynthesis
- Phosphorus compounds and reactions
- Catalytic Cross-Coupling Reactions
- Sphingolipid Metabolism and Signaling
- Multicomponent Synthesis of Heterocycles
- Crystallization and Solubility Studies
- Chemical Synthesis and Reactions
- X-ray Diffraction in Crystallography
- Malaria Research and Control
- Oxidative Organic Chemistry Reactions
- Synthesis of heterocyclic compounds
- Chemical Reaction Mechanisms
- Catalytic C–H Functionalization Methods
- Computational Drug Discovery Methods
- Marine Toxins and Detection Methods
- Bladder and Urothelial Cancer Treatments
- Cancer Treatment and Pharmacology
- Breast Cancer Treatment Studies
- Marine Sponges and Natural Products
Idorsia (Switzerland)
2023-2024
Actelion (Switzerland)
2016
University of Toronto
2016
University of Bern
2014
Universitäre Psychiatrische Dienste Bern
1987
The synthesis of substituted 2-cyclopentenones using a commercially available gold(I) catalyst is described under flexible reaction conditions. During the course our investigations, we discovered that proton source as an additive required to obtain desired cyclopentenones in good yields.
Piperidine
More than 40 % of the world's population is at risk being infected with malaria. Most malaria cases occur in countries sub-Saharan Africa, Central and South America, Asia. Resistance to standard therapy, including artemisinin combinations, increasing. There an urgent need for novel antimalarials new mechanisms action. In a phenotypic screen, we identified series phenylalanine-based compounds that exhibit antimalarial activity via yet unknown mechanism Our optimization efforts culminated...
In a prospective longitudinal study over several years, 58 patients with breast cancer are compared to 52 fibrocystic disease and 24 mastodynia. Results of coping (as assessed the Bernese Coping Modes) presented for illness course first 6 months: (1) There is considerable variation depending on situation state. A core group modes predominant in most situations: 'attention & care', 'problem analysis', 'Tackling'. average 10 different were used by per given situation. (2) The aspects (in same...
The development and execution of the large-scale synthesis LPA1-antagonist ACT-1016-0707 is described. Key developments were an improved nitrile hydrolysis, a high-yielding, safe, easy-to-perform amide coupling, isolation purification several, previously oily intermediates as crystalline solids. yield longest linear sequence nine steps was 34% on 450 g scale with respect to final product.
Abstract A general strategy for the synthesis of aignopsanes, a new family sesquiterpene natural products marine origin, is presented. The total (+)‐aignopsanoic acid ( 1 ), (−)‐methyl aignopsanoate 2 and (−)‐isoaignopsanoic 3 ) has been achieved their absolute configuration confirmed. (+)‐Microcionin‐1 4 structurally related furanosesquiterpene isolated in both enantiomeric forms from sponges, was also synthesized its established an unambiguous way. Interestingly, we report that...
Abstract Oxindoles are prevalent structures in natural products and pharmaceutically active molecules. To support structure–activity‐relationship (SAR) studies a medicinal chemistry program, we developed straightforward scalable synthesis route to 1‐aminoethyl oxindole building blocks harboring various types of substituents. Our strategy relies on an intramolecular Buchwald–Hartwig amidation 2‐bromophenylacetic amide precursor. The cyclization substrates can be prepared from readily...
The route scouting and development activities toward a safe scalable manufacturing for 3-(3-methoxyisoxazole-5-yl) propanoic acid are outlined in this article. In first step, methyl 3-hydroxy-5-isoxazolecarboxylate (CAS: 10068-07-2) was prepared on kilogram scale via bromination of dimethyl fumarate under photoflow conditions followed by condensation with hydroxyurea. This intermediate then two-carbon homologated sequence ester reduction, chlorination, nucleophilic substitution commercially...
Key words tandem catalysis - indanes indanones Heck cyclization
Key words donor–acceptor cyclobutanes - copper catalysis SaBOX oxazepanes
Key words cyclopropanation - electron-deficient olefins ruthenium catalysis
Key words glyoxylate-ene reaction - indium homoallylic alcohols PyBOX
Key words Heck–Matsuda reaction - cyclopentenediol desymmetrization stereoselectivity
Key words multicomponent reaction - amino acids copper rhodium