Combinatorial synthesis of small organic molecules

Angewandte Chemie (International Edition in English)

Volumn 35, Issue 20, 1996, Pages 2288-2337

  Balkenhohl, Friedhelm ^a   Von dem Bussche Hünnefeld, Christoph ^a   Lansky, Annegret ^a   Zechel, Christian ^a  

^a BASF SE   (Germany)

Author keywords

Automation; Combinatorial chemistry; Compound libraries; Molecular diversity; Solid phase synthesis

Indexed keywords

EID: 0030477258     PISSN: 05700833     EISSN: None     Source Type: Journal    
DOI: 10.1002/anie.199622881     Document Type: Article

References (25)

1. a) K. C. Nicolaou, E. Sorensen, Classics in Total Synthesis, Targets, Strategies, Methods, VCH, Weinheim, 1996
2. b) E. J. Corey, X.-M. Cheng, The Logic of Chemical Synthesis, Wiley, New York, 1989.
3. a) R. B. Silverman, J. Seydel, Medizinische Chemie, VCH, Weinheim, 1994
4. b) Medicinal Chemistry for the 21st Century (Ed.: C. G. Wermuth), Blackwell, Oxford, 1992.
5. General introductions: a) Combinatorial Libraries - Synthesis, Screening and Application Potential (Ed.: R: Cortese), Walter de Gruyter, Berlin, 1996 b) Combinatorial Libraries: The Theory and Practice of Combinatorial Chemistry (Ed.: R. A. Houghten), ESCOM, Leiden, 1995 c) Combinatorial Peptide and Non Peptide Libraries - a Handbook (Ed.: G. Jung), VCH, Weinheim, 1996 d) Molecular Diversity and Combinatorial Chemistry: Libraries and Drug Discovery (Eds.: I. Chaiken, K. Janda), ACS, Washington, 1996.
6. General introductions: a) Combinatorial Libraries - Synthesis, Screening and Application Potential (Ed.: R: Cortese), Walter de Gruyter, Berlin, 1996 b) Combinatorial Libraries: The Theory and Practice of Combinatorial Chemistry (Ed.: R. A. Houghten), ESCOM, Leiden, 1995 c) Combinatorial Peptide and Non Peptide Libraries - a Handbook (Ed.: G. Jung), VCH, Weinheim, 1996 d) Molecular Diversity and Combinatorial Chemistry: Libraries and Drug Discovery (Eds.: I. Chaiken, K. Janda), ACS, Washington, 1996.
7. General introductions: a) Combinatorial Libraries - Synthesis, Screening and Application Potential (Ed.: R: Cortese), Walter de Gruyter, Berlin, 1996 b) Combinatorial Libraries: The Theory and Practice of Combinatorial Chemistry (Ed.: R. A. Houghten), ESCOM, Leiden, 1995 c) Combinatorial Peptide and Non Peptide Libraries - a Handbook (Ed.: G. Jung), VCH, Weinheim, 1996 d) Molecular Diversity and Combinatorial Chemistry: Libraries and Drug Discovery (Eds.: I. Chaiken, K. Janda), ACS, Washington, 1996.
8. General introductions: a) Combinatorial Libraries - Synthesis, Screening and Application Potential (Ed.: R: Cortese), Walter de Gruyter, Berlin, 1996 b) Combinatorial Libraries: The Theory and Practice of Combinatorial Chemistry (Ed.: R. A. Houghten), ESCOM, Leiden, 1995 c) Combinatorial Peptide and Non Peptide Libraries - a Handbook (Ed.: G. Jung), VCH, Weinheim, 1996 d) Molecular Diversity and Combinatorial Chemistry: Libraries and Drug Discovery (Eds.: I. Chaiken, K. Janda), ACS, Washington, 1996.
9. The word "library" is not used consistently in the literature. Often the term library is reserved for substance mixtures whereas collections of single compounds are called "arrays".
10. The term combinatorial synthesis is strictly used only when different building blocks are treated in one reaction vessel, and mixtures are thus obtained. Since the boundary becomes blurred at the latest for the split synthesis (see refs. [13-15]), which also represents a compartmentalization ("one bead, one compound"), no differentiation will be made here.
11. a) H. M. Geysen, R. H. Meloen, S. J. Barteling, Proc. Natl. Acad. Sci. USA 1984, 81, 3998-4002
12. b) H. M. Geysen, S. J. Barteling, R. H. Meloen, ibid. 1985, 82, 178-182
13. c) N. J. Maeji, R. M. Valerio, A. M. Bray, R. A. Campbell, H. M. Geysen, Reactive Polymers 1994, 22, 203-212.
14. R. A. Houghten, Proc. Natl. Acad. Sci. USA 1985, 82, 5131-5135.
15. R. B. Merrifield, J. Am. Chem. Soc. 1963, 85, 2149-2154.
16. For the chemical synthesis of proteins, see E. Bayer, Angew. Chem. 1991, 103, 117-133; Angew. Chem. Int. Ed. Engl. 1991, 30, 113-129.
17. For the chemical synthesis of proteins, see E. Bayer, Angew. Chem. 1991, 103, 117-133; Angew. Chem. Int. Ed. Engl. 1991, 30, 113-129.
18. a) Reviews: G. Jung, A. G. Beck-Sickinger, Angew. Chem. 1992, 104, 375-391; Angew. Chem. Int. Ed. Engl. 1992, 31, 367-383
19. a) Reviews: G. Jung, A. G. Beck-Sickinger, Angew. Chem. 1992, 104, 375-391; Angew. Chem. Int. Ed. Engl. 1992, 31, 367-383
20. b) H.-E. Radunz, GIT Fachz. Lab. 1992, 869-873.
21. R. Frank, Tetrahedron 1992, 48, 9217-9232.
22. VLSIPS: very large scale immobilized polymer synthesis (photolithographic parallel synthesis); S. P. A. Fodor, J. L. Read, M. C. Pirrung, L. Stryer, A. T. Lu, D. Solas, Science 1991, 251, 767-773.
23. "Studies on Possibilities of Systematic Searching for Pharmaceutically Useful Peptides": A. Furka, notarized Document No. 36237/1982, Budapest, 1982.
24. a) A. Furka, F. Sebestyen, M. Asgedom, G. Dibo, Abstr. 14th Int. Congr. Biochem., Prague, 1988, 5, 47
25. b) Abstr. 10th Int. Symp. Med. Chem., Budapest, 1988, 9, 288.