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A novel method synthesizes isoindolinones via tandem reactions in a simple and efficient manner, highlighting practical applications.
Isoindolinones are essential heterocycles with wide-ranging biological activities and medicinal values, and therefore, efficient approaches to their synthesis remain in demand. Herein, a novel and operationally simple method to generate isoindolinones is reported by using a tandem reaction of N-methylbenzylamines and methyl 2-fluorobenzoates mediated by LiN(SiMe₃)₂ and CsF systems (33 examples, 30-85% yields). The synthesis of C3-quaternary isoindolinone further demonstrated the potential practicality of these tandem reactions.
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Ma et al. (2026) studied this question.
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