Facile preparation of 6-(Aminomethyl)isoindolin-1-one realizing complete reduction of double aromatic cyano groups
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 analogue, is synthesized via this route as well.
Bi, Lei,Fu, Chenchao,Yao, Lei
p. 6655 - 6657
(2015/02/19)
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