One-Pot Synthesis of Indolin-3-ones Mediated by LiN(SiMe3)2/CsF

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.