ABSTRACT
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The rapid assembly of “drug-like” core templates is fundamental to the discovery phase of many medicinal chemistry programs. Provided that the syntheses of these core templates will allow for their ready functionalization, a meaningful SAR (structure-activity relationship) study can be efficiently conducted. In addition to ready assembly and core functionalization, the core template should have relatively low molecular weight and log P.1 This will allow room for the molecule to “grow” as functionalization is incorporated, thus allowing the targeting of the many essential criteria of drug candidates including selectivity, potency, and efficacy. Combinatorial technology is at the forefront of medicinal chemistry and is receiving widespread attention as a powerful tool in drug discovery.2 Many of the approaches devised to prepare such libraries rely on solid-phase synthesis techniques and exploit the efficient split/pool and parallel methods to assemble a statistical sampling of all possible combinations of a set of chemical building blocks.
