Highly enantioselective organocatalytic synthesis of piperidines. Formal synthesis of (−)-Paroxetine

A highly enantioselective organocatalytic synthesis of piperidines is reported. The reaction is catalyzed by simple and commercially available secondary amines, affording the corresponding adducts with high yields and enantioselectivities. Moreover, this reaction is used for the formal synthesis of (−)-Paroxetine, a blockbuster drug, in only three steps.

Graphical abstractFigure optionsDownload full-size imageDownload as PowerPoint slide