One-Pot Synthesis of Indolin-3-ones Mediated by LiN(SiMe3)2/CsF
Ruyuan Ma1, Yuanyun Gu1, Yan-En Wang2
1School of Chemistry and Molecular Engineering, Nanjing Tech University, 30 South Puzhu Road, Nanjing 211816, P. R. China.
Organic Letters
|June 7, 2024
Abstract:
Indolin-3-ones 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 indolin-3-ones is reported by using a tandem reaction of N-methylbenzylamines and methyl 2-fluorobenzoates mediated by the LiN(SiMe3)2 and CsF system (34 examples, 30-85% yields). The synthesis of C2-quaternary indolin-3-one further demonstrated the potential practicability of these tandem reactions.
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