TLC used as tool for combinatorial synthesis

A process that combines synthesis, separation, analysis, and screening on a thin-layer chromatography (TLC) plate could be exploited for the preparation and biological screening of combinatorial libraries of compounds, according to chemists in Norway. The process was developed by a group led by research scientist Lorenzo Williams at SINTEF Applied Chemistry, a research institute located in Oslo and Trondheim. The chemists carried out the parallel synthesis of a number of sulfonamides by reaction of various arylpiperazines with sulfonyl halides and showed that the reaction can be optimized rapidly on a glass TLC plate coated with silica gel. They then demonstrated that the sulfonamides can be screened on the plate for antimicrobial activity against bacteria. "The system provides a simple and cost-effective method for performing four processes sequentially on the same reaction medium without the need for undesirable chemical manipulations or further handling," Williams tells C&EN. "One can rapidly optimize ...