Catalytic Asymmetric Construction of Chiral Indoloazepine-Based Spirooxindoles via Formal [6+1] Cycloadditions
The first chiral phosphoric acid-catalyzed formal [6+1] cycloaddition of (2-aminobenzyl)indoles with isatins has been developed, efficiently affording biologically important chiral indoloazepine-based spirooxindoles in high yields (up to 99%) and excellent enantioselectivities (up to 97:3 er). Notably, this novel class of chiral indoloazepine-based spirooxindoles exhibits potent cytotoxicity against human liver cancer cell line HepG2.
Authors
- Xueting Liu (ORCID: https://orcid.org/0000-0002-0585-0472)
- Shuang Yang (ORCID: https://orcid.org/0000-0002-5573-5632)
- Tianzi Huang
- Xiao-Qin Shi
- Tian-Shu Zhang
- Shuai Liu
- Hua Sun
Institutions
- Xuzhou University of Technology (CN)
- Zhengzhou University (CN)
- Jiangsu University of Science and Technology (CN)
Publication Details
- Journal
- Organic Letters
- Published
- 2026-04-06
- DOI
- https://doi.org/10.1021/acs.orglett.6c00948
- Primary Topic
- Synthesis and pharmacology of benzodiazepine derivatives
- Type
- article
- Field-Weighted Citation Impact
- 0.00
Funders
- Natural Science Foundation of Jiangsu Province
- Xuzhou Science and Technology Bureau