ABSTRACT
In the process of identifying new compounds with interesting properties, combi natorial chemistry (CC) has proven its value. These properties may lie in the area of new pharmaceuticals, novel materials, artificial enzymes, catalysts, surfactants, etc. In the pharmaceutical field, CC started with the generation of huge libraries of non-druglike compounds such as peptide oligomers, generally considered to be poor as drug candidates or even as leads. The pharmaceutical industry quickly understood that they had to focus on “ good quality” compounds-compounds that were amenable to optimization toward more druglike behavior. Therefore, in the last few years CC methodology has been increasingly aimed at the synthesis of small organic molecules. Although more and more classical organic reactions are being adapted for solid-phase reactions (1-6) it has to be accepted that even with today’s available repertoire only a small portion of the diversity space can be addressed. What is even more frustrating is that most of the time we are fishing in the same pond. Therefore, the synthesis of “ good quality” compounds is rely ing heavily on the identification of new robust solid-phase or solution-phase pro cesses.
