RPR's approach to high-speed parallel synthesis for lead generation

Rhone-Poulene Rorer (RPR) is developing high-speed parallel synthesis as an essential tool to produce large libraries for lead generation. Libraries of 5000-10,000 members are produced as singles by solution- or solid-phase chemistry for screening in high-throughput assays in order to foster lead generation and accelerate lead optimization. Libraries are designed to optimize chemical diversity by applying a combination of virtual selection methods. The author describes how, in spite of different 2D structural features, library compounds share most of the 'drug-like' properties of compounds from the MDL Drug Data Report database, in terms of pharmacophore coverage and atomic and molecular properties.