Catalytic Asymmetric Construction of Chiral Indoloazepine-Based Spirooxindoles via Formal [6+1] Cycloadditions

Organic Letters 2026

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Authors: Qiong Wu, Shuang Yang, Tianzi Huang, Shuai Liu, Xiao-Qin Shi, Hua Sun, Tian-Shu Zhang, Jia-Jia Zhao, Xueting Liu
DOI: 10.1021/acs.orglett.6c00948
Cited by: 3
References: 48

Abstract

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.

Fields of Study & Subjects

Synthesis and pharmacology of benzodiazepine derivatives Asymmetric Synthesis and Catalysis Synthesis and bioactivity of alkaloids

Publication details

Journal / source
Organic Letters
Publisher
American Chemical Society (ACS)
Volume
28
Issue
15
Pages
4887–4892
Publication date
6 April 2026
Language
EN