Strategy and Tactics in Combinatorial Organic Synthesis. Applications to Drug Discovery


  • Eric M. Gordon
  • Dinesh V. Patel
  • Jeffrey W. Jacobs
  • Mikhail F. Gordeev
  • Joseph Zhou




A strategic analysis of various issues which pertain to the enablement of combinatorial organic synthesis to produce libraries of non-polymeric organic molecules is given. Methods and examples of the development of solid-phase organic chemistry and its subsequent application to combinatorial library synthesis for drug discovery is illustrated with successful case studies. The synthetic versatility of resin-bound amino-acid-derived imine intermediates to produces, β-sultams and pyridines is shown. Use of natural products as key components for creation of combinatorial libraries is presented using Rauwolfia alkaloids and the cephalosporin nucleus as examples.




How to Cite

E. M. Gordon, D. V. Patel, J. W. Jacobs, M. F. Gordeev, J. Zhou, Chimia 1997, 51, 821, DOI: 10.2533/chimia.1997.821.