1-Aryl-3,4-dihydro-1H-quinolin-2-one derivatives, novel and selective norepinephrine reuptake inhibitors

A novel series of 1-aryl-3,4-dihydro-1H-quinolin-2-ones have been discovered as potent and selective norepinephrine reuptake inhibitors. Efficient synthetic routes have been developed which allow for the multi-gram preparation of both final targets and advanced intermediates for SAR expansion.

Graphical abstractA novel series of 1-aryl-3,4-dihydro-1H-quinolin-2-ones has been discovered as potent and selective norepinephrine reuptake inhibitors. Efficient synthetic routes have been developed, which allow for the multi-gram preparation of both final targets and advanced intermediates for SAR expansion.Figure optionsDownload full-size imageDownload as PowerPoint slide