Modification of the clozapine structure by parallel synthesis

A structure–activity study based on the core structure of clozapine 1b was accomplished by utilizing high-throughput synthesis. Several focused libraries were designed and synthesized to quickly develop SAR. The results indicate that by varying different regions of clozapine, both D1-selective and D2-selective compounds can be obtained.

Graphical abstractThe structure of clozapine was modified to provide two series of compounds that displayed high selectivity for either the dopamine D1 or D2 receptor.Figure optionsDownload full-size imageDownload as PowerPoint slide