Cobalt-Catalyzed Cascade Synthesis of 5-Amino-1,2,4-triazolo[1,5-<i>c</i>]quinazoline Derivatives via Multiple C–N Bonds Construction

A cobalt-catalyzed three-component cascade reaction for the synthesis of functionalized 5-amino-1,2,4-triazolo[1,5-<i>c</i>]quinazoline derivatives is presented. The reaction involves <i>ortho</i>-cyanoaryl isocyanides, azides, and hydrazides, giving products in good to excellent yields. The protocol is highly scalable, as demonstrated by a gram-scale reaction of bioactive CGS-15943, providing a robust, efficient method for synthesizing triazoloquinazoline derivatives and offering significant potential for drug discovery and further modifications.

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Publication Details

Journal
The Journal of Organic Chemistry
Published
2025-05-28
DOI
https://doi.org/10.1021/acs.joc.5c00658
Primary Topic
Quinazolinone synthesis and applications
Type
article
Field-Weighted Citation Impact
0.00

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article

Cobalt-Catalyzed Cascade Synthesis of 5-Amino-1,2,4-triazolo[1,5-c]quinazoline Derivatives via Multiple C–N Bonds Construction

Xiaoping Xu, You Zi, Sifan Wu, Shun‐Jun Ji et al.
The Journal of Organic Chemistry
Quinazolinone synthesis and applications
article

Cobalt-Catalyzed Cascade Synthesis of 5-Amino-1,2,4-triazolo[1,5-c]quinazoline Derivatives via Multiple C–N Bonds Construction

Xiaoping Xu, You Zi, Sifan Wu, Shun‐Jun Ji, Zhengkun Li
article en

Abstract

A cobalt-catalyzed three-component cascade reaction for the synthesis of functionalized 5-amino-1,2,4-triazolo[1,5-<i>c</i>]quinazoline derivatives is presented. The reaction involves <i>ortho</i>-cyanoaryl isocyanides, azides, and hydrazides, giving products in good to excellent yields. The protocol is highly scalable, as demonstrated by a gram-scale reaction of bioactive CGS-15943, providing a robust, efficient method for synthesizing triazoloquinazoline derivatives and offering significant potential for drug discovery and further modifications.

The Journal of Organic ChemistryVol. 90(22)
Nantong University (CN), Soochow University (CN), Laboratoire de Synthèse Organique (FR)
National Natural Science Foundation of China, Natural Science Foundation of Jiangsu Province, Priority Academic Program Development of Jiangsu Higher Education Institutions
Openalex Percentile: Top 91%
Quinazolinone synthesis and applications
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Cobalt-Catalyzed Cascade Synthesis of 5-Amino-1,2,4-triazolo[1,5-<i>c</i>]quinazoline Derivatives via Multiple C–N Bonds Construction — Xiaoping Xu, You Zi, et al. · The Journal of Organic Chemistry (2025) | TGRS Research Map | TGRS