A5050093185- Chemical Synthesis and Analysis
- Cyclopropane Reaction Mechanisms
- Chemical Synthesis and Reactions
- Synthetic Organic Chemistry Methods
- Crystallography and molecular interactions
- Synthesis and Catalytic Reactions
- Crystallization and Solubility Studies
- X-ray Diffraction in Crystallography
- Synthesis and Reactivity of Sulfur-Containing Compounds
- Click Chemistry and Applications
- Fluorine in Organic Chemistry
- Synthesis and Biological Evaluation
- Asymmetric Hydrogenation and Catalysis
- Asymmetric Synthesis and Catalysis
- Sulfur-Based Synthesis Techniques
- Catalytic Cross-Coupling Reactions
- Organometallic Complex Synthesis and Catalysis
- Supramolecular Chemistry and Complexes
- Mast cells and histamine
- Synthesis and Reactions of Organic Compounds
- Synthesis and Biological Activity
- Inorganic Fluorides and Related Compounds
- Synthesis and Characterization of Heterocyclic Compounds
- Advanced Synthetic Organic Chemistry
- Multicomponent Synthesis of Heterocycles
Lonza (Switzerland)
2010-2020
Novo Nordisk (Denmark)
1997-2011
University of North Texas
1993-1996
Technische Universität Dresden
1995
Abstract The CF 3 group is an omnipresent motif found in many pharmaceuticals, agrochemicals, catalysts, materials, and industrial chemicals. Despite well‐established trifluoromethylation methodologies, the straightforward selective introduction of such groups into (hetero)arenes using available less expensive sources still a major challenge. In this regard, synthesis various trifluoromethyl‐substituted by palladium‐catalyzed C−H functionalization herein reported. This novel methodology...
Abstract The CF 3 group is an omnipresent motif found in many pharmaceuticals, agrochemicals, catalysts, materials, and industrial chemicals. Despite well‐established trifluoromethylation methodologies, the straightforward selective introduction of such groups into (hetero)arenes using available less expensive sources still a major challenge. In this regard, synthesis various trifluoromethyl‐substituted by palladium‐catalyzed C−H functionalization herein reported. This novel methodology...
ADVERTISEMENT RETURN TO ISSUECommunicationNEXTResin-Bound Isothiocyanates and Their Synthetic Equivalents as Intermediates for the Solid-Phase Synthesis of Substituted ThiophenesHenrik Stephensen Florencio ZaragozaView Author Information Novo Nordisk A/S, Park, DK-2760 Måløv, DenmarkCite this: J. Org. Chem. 1997, 62, 18, 6096–6097Publication Date (Web):September 5, 1997Publication History Received23 May 1997Published online5 September inissue 1...
ADVERTISEMENT RETURN TO ISSUEPREVNoteNEXTSolid-Phase Synthesis of Substituted 4-Acyl-1,2,3,4-tetrahydroquinoxalin-2-onesFlorencio Zaragoza and Henrik StephensenView Author Information Novo Nordisk A/S, Park, DK-2760 Måløv, Denmark Cite this: J. Org. Chem. 1999, 64, 7, 2555–2557Publication Date (Web):March 11, 1999Publication History Received14 October 1998Published online11 March 1999Published inissue 1 April...
Fluoroalkylated olefins made easy: a mild and selective Ni-catalyzed fluoroalkylation including trifluoromethylation of alkenes was developed. Various fluorinated were provided in good to excellent yields.
New traceless linkers based on sulfur and selenium mediate useful chemical transformations of substrates during their attachment to solid supports. Also, the cleavage from support can now be performed with simultaneous C−C bond formation. A cyclization selenium-functionalized polystyrene (Pol) is shown.
ADVERTISEMENT RETURN TO ISSUEPREVNoteNEXT(Cyanomethyl)trialkylphosphonium Iodides: Efficient Reagents for the Intermolecular Alkylation of Amines with Alcohols in Solution and on Solid PhaseFlorencio Zaragoza Henrik StephensenView Author Information Novo Nordisk A/S, Park, DK-2760 Måløv (Denmark) [email protected]Cite this: J. Org. Chem. 2001, 66, 7, 2518–2521Publication Date (Web):March 10, 2001Publication History Received13 December 2000Published online10 March 2001Published inissue 1...
With the aim of identifying structurally novel, centrally acting histamine H(3) antagonists, a series 2-(4-alkylpiperazin-1-yl)quinolines was prepared. Systematic variation substituents led to highly potent antagonists with low polar surface area and appropriate log P for blood-brain barrier penetration.
With the aim of identifying structurally novel, centrally acting histamine H(3) antagonists, arrays monoacyldiamines were screened. This led to discovery a series 1-alkyl-4-acylpiperazines which potent antagonists at human receptor. The most amides had antagonist potencies in subnanomolar range.
Polyfunctionalized, unprotected reagents (e.g. amines and thiols) can be used in the production of highly diverse compound libraries by performing sequential nucleophilic substitutions on support-bound polyelectrophiles (see scheme). The procedure reported here enables efficient preparation new beta-alanine derivatives which are suitable for lead discovery. E*=polyelectrophile, *=solid support.
Treatment of alcohols with an excess (cyanomethyl)trimethylphosphonium iodide leads, after aqueous hydrolysis, to the clean formation nitriles two more carbon atoms than present in original alcohol. Benzylic, allylic, and aliphatic without beta-branching (RCH(2)CH(2)OH) have been converted success. The required phosphonium is simple prepare can be stored for a long time at room temperature.
Treatment of aromatic and heteroaromatic methyl ketones with sulfur monochloride catalytic amounts pyridine in refluxing chlorobenzene leads to the formation acyl chlorides. Both electron-rich electron-poor aryl can be used as starting materials. The resulting C1-byproduct depends on precise reaction conditions chosen.