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Updated: Dec 27, 2025

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
Published on: February 9, 2021
Efficient synthesis of SCF3-substituted tryptanthrins by a radical tandem cyclization
Jincheng Guo1, Yanan Hao1, Gang Li1
1State Key Laboratory of Elemento-Organic Chemistry, Research Institute of Elemento-Organic Chemistry, College of Chemistry, Collaborative Innovation Center of Chemical Science and Engineering (Tianjin), Nankai University, Tianjin 300071, China. wangqm@nankai.edu.cn liuyuxiu@nankai.edu.cn.
Abstract:
Herein, we report a new, efficient and atom-economical strategy for the synthesis of SCF3-substituted tryptanthrin derivatives. These previously unreported derivatives were obtained by means of a radical tandem cyclization. The reaction was triggered by addition of a SCF3 radical to a carbon-carbon double bond and involved the formation of a C(sp3)-SCF3 bond, a C(sp2)-C bond, and a C(sp2)-N bond. This method has mild conditions and a wide range of substrates which is particularly useful for the preparation of substituted indolquinazoline derivatives that widely exist in many natural products, but are not easy to obtain by conventional approaches.
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