STRATEGY AND TACTICS IN COMBINATORIAL ORGANIC-SYNTHESIS - APPLICATIONS TO DRUG DISCOVERY

A strategic analysis of various issues which pertain to the enablement of combinatorial organic synthesis to produce libraries of non-polyme ric organic molecules is given. Methods and examples of the developmen t of solid-phase organic chemistry and its subsequent application to c ombinatorial library synthesis for drug discovery is illustrated with successful case studies. The synthetic versatility of resin-bound amin o-acid-derived imine intermediates to produces beta-sultams and pyridi nes is shown. Use of natural products as key components for creation o f combinatorial libraries is presented using Rauwolfia alkaloids and c ephalosporin nucleus as examples.