One-Pot Synthesis of Isoindolinones Mediated by LiN(SiMe <sub>3</sub> ) <sub>2</sub> /CsF
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 <i>N</i>-methylbenzylamines and methyl 2-fluorobenzoates mediated by LiN(SiMe<sub>3</sub>)<sub>2</sub> and CsF systems (33 examples, 30-85% yields). The synthesis of C3-quaternary isoindolinone further demonstrated the potential practicality of these tandem reactions.
Authors
- Yuanyun Gu (ORCID: https://orcid.org/0000-0002-7868-0822)
- Rongbi Fei
- Jianyou Mao
- Yan-En Wang
- Dan Xiong
- Ruyuan Ma
Institutions
- Hebei Agricultural University (CN)
- Nanjing Tech University (CN)
Publication Details
- Journal
- Organic Letters
- Published
- 2026-02-13
- DOI
- https://doi.org/10.1021/acs.orglett.5c01728
- Primary Topic
- Synthesis and pharmacology of benzodiazepine derivatives
- Type
- article
- Field-Weighted Citation Impact
- 0.00