Facile Preparation of 6-(Aminomethyl)isoindolin-1-one Realizing Complete Reduction of Double Aromatic Cyano Groups

摘要

6(Aminomethyl)isoindolin-1-one is a key intermediate enroute to many investigational therapeutic agents. The need for it prompts a concise synthesis, which includes; (1) cyanation without using costly transition metal catalysts; (2) complete hydrogenation of the resulting dicyanide. This synthetic route emphasizes high atom-efficiency and simple operation. 5-(Aminomethyl)isoindolin-1-one. a structural malogue, is synthesized via this route as well.