CHIMIA (Nov 1997)

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

Journal volume & issue
Vol. 51, no. 11

Abstract

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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, ?-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.