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Published on: September 6, 2019
One-Pot Synthesis of Isoindolinones Mediated by LiN(SiMe3)2/CsF
Ruyuan Ma1, Yuanyun Gu1, Yan-En Wang2
1State Key Laboratory of Materials Oriented Chemical Engineering (MCE), Technical Institute of Fluorochemistry (TIF), School of Chemistry and Molecular Engineering, Nanjing Tech University, 30 South Puzhu Road, Nanjing 211816, P. R. China.
None:
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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