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Tryptophan-derived butyrylcholinesterase inhibitors as promising leads against Alzheimer's disease.
We have identified tryptophan-based selective nanomolar butyrylcholinesterase (BChE) inhibitors. They are defined according to their chemical modularity, novel binding mode revealed by five solved
Structures of the Reactive Intermediates in Organocatalysis with Diarylprolinol Ethers
Structures of the reactive intermediates (enamines and iminium ions) of organocatalysis with diarylprolinol derivatives have been determined. To this end, diarylprolinol methyl and silyl ethers, 1,
Isolation and X-Ray Structures of Reactive Intermediates of Organocatalysis with Diphenylprolinol Ethers and with Imidazolidinones
Reaction of 2-phenylacetaldehyde with the Me3Si ether of diphenyl-prolinol, with removal of H2O, gives a crystalline enamine (1). The HBF4 salts of the MePh2Si ether of diphenyl-prolinol and of
Enantioselective Preparation of ߲-Amino Acid Derivatives for -Peptide Synthesis
β-Amino acids with a single side chain in the α-position (β 2 -aminoacids or H-β 2 -aminoacids or H-β 2 hXaa(PG)-OH; i.e., homo-aminoacids with proteinogenic side chains) have turned out to be
Recent Advances in the Synthesis of Polysubstituted 3-Pyrazolidinones
An account of recent developments in the field of 3-pyrazolidinone chemistry is given with special focus on the synthesis and transformations of 5-substituted
Stereochemical Models for Discussing Additions to α,β-Unsaturated Aldehydes Organocatalyzed by Diarylprolinol or Imidazolidinone Derivatives - Is There an '(E)/(Z) -Dilemma'?
The structures of iminium salts formed from diarylprolinol or imidazolidinone derivatives and α,β-unsaturated aldehydes have been studied by X-ray powder diffraction (Fig. 1), single-crystal X-ray
Metal-catalyzed [3+2] cycloadditions of azomethine imines
In the last decade, metal-catalyzed [3+2] cycloadditions of azomethine imines have emerged as a regioselective and stereoselective method for the synthesis of pyrazolidines and pyrazolines. A
"Click" Chemistry: Application of Copper Metal in Cu-Catalyzed Azomethine Imine-Alkyne Cycloadditions.
The availability of azomethine imines, mild reaction conditions, simple workup, and scalability make CuAIAC a viable supplement to the Cu-catalyzed azide-alkyne cycloaddition reaction in "click" chemistry.