Characterization of Spatially Addressable Libraries: Stereoisomer Analysis of Tetrahydro-#beta#-carbolines as an Example

摘要

Combinatorial chemistry approaches have facilitated the process of lead discovery and optimization for new drugs, catalysts, and materials. A successful combinatorial program typically includes high throughput library synthesis, characterization, and screening. One of many challenges in this program is to develop high throughput characterization methods to address issues concerning reaction stereoselectivity and racemization during the library synthesis. Using the core structure of tetrahydro-#beta#-carboline as an example, we demonstrate the usefulness of capillary electrophoresis in enantiomeric separation of stereoisomers generated by parallel synthesis and rapid quantitative measurement of the isomer ratios, in addition to assessing possible racemization during reactions for its overall potential in library characterization.