Abstract
Disclosed herein is an expedient synthesis of biologically important isoindolinone derivatives from reactions of 2-formylbenzoic acids with various amines. This method operates via a deliberately designed catalyst-free tandem reductive amination/cyclization cascade event triggered by a transfer hydrogenation process with easily available Hantzsch ester as the organic hydride source. The ease of operation, mild reaction conditions, facile accessibility of the starting materials, and easy scalability of the current method distinguish it from the other precedent protocols, thus enable it a practical approach to the syntheses of valuable isoindolinone-incorporated drugs.
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