I<sub>2</sub>-Mediated [3 + 3] Annulation for the Construction of Indole-Pyrimidine-Pyrazole-Fused Tetracyclic Heteroarenes

An I<sub>2</sub>-mediated annulation of 3-aminopyrazoles with indole-3-carboxaldehydes has been demonstrated for the first time. This tandem strategy allows the facile construction of indole-pyrimidine-pyrazole-fused tetracyclic heteroarenes that are otherwise inaccessible by the existing methods. These fused heterocycles exhibited enhanced antifungal activities against <i>Valsa mali</i> and <i>Botryosphaeria dothidea</i> compared with commercial Xemium fungicide.

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Publication Details

Journal
The Journal of Organic Chemistry
Published
2024-10-07
DOI
https://doi.org/10.1021/acs.joc.4c01934
Citations
3
Primary Topic
Catalytic C–H Functionalization Methods
Type
article
Field-Weighted Citation Impact
0.75

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article

I2-Mediated [3 + 3] Annulation for the Construction of Indole-Pyrimidine-Pyrazole-Fused Tetracyclic Heteroarenes

Kun Xu, Heng-Tong Qu, Cheng‐Tao Feng, Jiaxin Yang et al.
3 citations
The Journal of Organic Chemistry
Catalytic C–H Functionalization Methods
0.75
article

I2-Mediated [3 + 3] Annulation for the Construction of Indole-Pyrimidine-Pyrazole-Fused Tetracyclic Heteroarenes

Kun Xu, Heng-Tong Qu, Cheng‐Tao Feng, Jiaxin Yang, Fan Teng, Jia-Hui Hong, Long-Sheng Zhou
article en
3 citations

Abstract

An I<sub>2</sub>-mediated annulation of 3-aminopyrazoles with indole-3-carboxaldehydes has been demonstrated for the first time. This tandem strategy allows the facile construction of indole-pyrimidine-pyrazole-fused tetracyclic heteroarenes that are otherwise inaccessible by the existing methods. These fused heterocycles exhibited enhanced antifungal activities against <i>Valsa mali</i> and <i>Botryosphaeria dothidea</i> compared with commercial Xemium fungicide.

The Journal of Organic ChemistryVol. 89(20)
Anhui University of Traditional Chinese Medicine (CN), Beijing University of Technology (CN), Shandong Academy of Chinese Medicine (CN)
National Natural Science Foundation of China, Anhui Provincial Department of Education, Natural Science Foundation of Anhui Province, Beijing Municipal Natural Science Foundation
Zero hunger
Openalex Percentile: Top 32%
Catalytic C–H Functionalization Methods
0.75
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I<sub>2</sub>-Mediated [3 + 3] Annulation for the Construction of Indole-Pyrimidine-Pyrazole-Fused Tetracyclic Heteroarenes — Kun Xu, Heng-Tong Qu, et al. · The Journal of Organic Chemistry (2024) | TGRS Research Map | TGRS