Combinatorial Chemistry: Methods and Trends

With combinatorial chemistry millions of organic compounds, peptide mimetics and oligomers can be produced simultaneously and quickly. These compound libraries are a cost-effective resource for the pharmaceutical industry in their search for biologically active lead structures. Simultaneous parallel multi-step syntheses including most of the common organic reactions can be carried out in novel reactors and with automated methods based on reproducible techniques developed for organic chemistry on solid supports (1-4). Fast and efficient analytical on- and off-bead techniques are essential for various synthetic approaches and technologies, characterizing the products of high molecular diversity and detecting by-products. HPLC-MS, FT-ATR-IR, gel-phase and MAS-NMR are used and no tagging is required. Screening assays in solution and on microstructured surfaces are an indispensible source of leads and fundamental structure activity relationships for every researcher in this rapidly developing field, which spans biochemistry, biotechnology, pharmaceutical, medicinal and organic chemistry.

Selected Publications

1. G. Jung and A. G. Beck-Sickinger (1992).
Multiple Peptide Synthesis Methods and Their Applications, Angew. Chem. 104, 375-391; Angew. Chem. Int. Ed. Engl. 31, 367-383.

2. G. Jung (ed.) (1996).
Combinatorial Peptide and Non-peptide Libraries (566 pages, 214 figures, 73 tables), Verlag Chemie, Weinheim.

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

4. J. Früchtel and G. Jung (1996)
Organic Chemistry on Solid Supports - Basic Principles for Combinatorial Chemistry - A Review in: G.Jung (ed.), Combinatorial Peptide and Nonpeptide Libraries, pp. 19-78, Verlag Chemie, Weinheim.

5. W.J. Haap, T. Redemann, J.S. Früchtel, and G. Jung (1997)
Analytical Methods in Combinatorial Chemistry: FT-IR Spectroscopy, ATR-Spectroscopy and IR-Microscopy, GIT, Special Edition April 1997, 94-98.

6. W.J.Haap, J.W. Metzger, C. Kempter, and G. Jung (1997)
Composition and Purity of Combinatorial Aryl Ether Collections analyzed by Electrospray Mass Spectrometry, Mol. Diversity, accepted for publication.

cojinfo@uni-tuebingen.de(cojinfo@uni-tuebingen.de) - July 23, 1997