Synthesis and solid-phase purification of anthranilic sulfonamides as CCK-2 ligands

A novel strategy for the synthesis of cholecystokinin-2 receptor ligands was developed. The route employs a solution-phase synthesis of a series of anthranilic sulfonamides followed by a resin capture purification strategy to produce multi-milligram quantities of compounds for bioassay. The synthesis was used to produce >100 compounds containing various functional groups, highlighting the general applicability of this strategy and to address specific metabolism issues in our CCK-2 program.

Graphical abstractA novel strategy for the library synthesis of cholecystokinin-2 receptor ligands was developed to rapidly address ligand metabolism issues which employed a solution-phase sulfonamide synthesis, followed by a resin capture purification methodology.Figure optionsDownload full-size imageDownload as PowerPoint slide