Preparative LC/MS Technology: A Key Component of the Existing High Speed Synthesis Platform at Syngenta

Abstract

Sizable investments in laboratory automation and state-of-the-art purification equipment were made at Syngenta Crop Protection with the objective to increase synthesis capacity and effectively support typical lead optimization activities. The successful implementation of a high-speed-synthesis platform consisted of the modular assembly of various commercially available liquid-handling workstations in combination with in-house developed parallel synthesis reaction manifolds. Preparative LC/MS technology was identified as a key success factor for optimizing overall throughput by addressing existing bottlenecks in parallel synthesis such as the fast and unattended isolation of compounds. Automated data analysis is crucial for high-throughput quality control and to allow all compounds of interprets to be sorted rapidly, i.e. those having defined structures and passing predefined purity criteria. The integrated application of the tools as described is intended to support chemists in their task to derive reliable structure–activity relationships more quickly and hopefully to shorten the time needed to identify innovative drug candidates.