Combinatorial organic chemistry

Methods for the parallel multiple synthesis of thousands of organic small molecules with hundreds of diverse scaffolds were developed based on our extensive experiences in combinatorial solid phase synthesis. Large collections of single, analytically well-defined heterocyclic compounds were produced on novel and optimized solid supports and linkers. Validated process acceleration by automation, high yields and purity as well as perfect on- and off-bead analyses were in our permanent focus during our micro- and macroscale organic syntheses for the lead finding and optimization process.

J. Früchtel and G. Jung (1996). Organic Chemistry on Solid Supports, Angew. Chem. 108, 19-46; Angew. Chem. Int. Ed. Engl. 35, 17-42

G. Jung (ed.) (1996). Combinatorial Peptide and Nonpeptide Libraries, 18 chapt., 544 pp.; VCH Verlagsgesellschaft, Weinheim

G. Jung, H. Hofstetter, S. Feiertag, D. Stoll, O. Hofstetter, K.H. Wiesmüller, and V. Schurig (1996). Cyclopeptide Libraries as New Chiral Selectors in Capillary Electrophoresis, Angew. Chem. 108, 2261-2263; Angew. Chem. Int. Ed. Engl. 35, 2148-2150.

W.J. Haap, T. Walk, and G. Jung (1998). FT-IR Mapping – A New Tool for Spatially Resolved Characterization of Polymer Bound Combinatorial Compound Libraries with IR-Microscopy, Angew. Chem. 110, 3506-3509; Angew. Chem. Int. Ed. Engl. 37, 3311-3314

G. Jung (ed.) (1999). Combinatorial Chemistry, Synthesis, Analysis, Screening, 20 chapt., 601 pp.; Wiley-VCH Verlag, Weinheim

J. Rademann and G. Jung (2000). Integrating Combinatorial Synthesis and Bioassays, Science 287, 1947-1948

H. Eickhoff, A. Rieker, and G. Jung (2001). Oxidative Phenol Coupling – Tyrosine Dimers and Libraries Containing Tyrosyl Peptide Dimers, Tetrahedron 57, 353-364

J. Rademann, J. Smerdka, G. Jung, P. Grosche, and D. Schmid (2001). Alkylating Polymers: Resin-Released Carbenium Ions as Versatile Reactive Intermediates in Polymer-Assisted Solution-Phase Synthesis, Angew. Chem. 113, 390-393; Angew. Chem. Int. Ed. Engl. 40, 381-385

S. Weik, G. Nicholson, G. Jung and J. Rademann (2001). Oxoammonium Resins as Metal-free, Highly Reactive, Versatile Polymeric Oxidative Reagents, Angew. Chem. 113, 1489-1492; Angew. Chem. Int. Ed. Engl. 40, 1436-1439

G. Sorg, A. Mengel, G. Jung, and J. Rademann (2001). Oxidizing Polymers: A Polymer-Supported, Recyclable Hypervalent Iodine (V) Reagent for the Efficient Conversion of Alcohols, Carbonyl Compounds, and Unsaturated Carbamates in Solution, Angew. Chem. 113, 4532-4535; Angew. Chem. Int. Ed. Engl. 40, 4395-4397

D.G. Schmid, P. Grosche, and G. Jung (2001). High-Resolution Analysis of a 144-Membered Pyrazole Library from Combinatorial Solid Phase Synthesis by using Electrospray Ionisation Fourier Transform Ion Cyclotron Resonance Mass Spectrometry, Rapid Commun. Mass Spectrom. 15, 341-347

J. Rademann, M. Barth, R. Brock, H.-J. Egelhaaf, and G. Jung (2001). Spatially Resolved Single Bead Analysis: Homogeneity, Diffusion, and Adsorption in Cross-Linked Polystyrene, Chem. Eur. J. 7, 3884-3889

Diverse compound collections for the drug finding process (EMC microcollections)

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