Three-Component Tandem Annulation for the Synthesis of Pyrido[4,3- <i>d</i> ]pyrimidine-2,4-diones

An efficient catalyst- and base-free, three-component tandem annulation has been developed for the synthesis of pyrido[4,3-<i>d</i>]pyrimidine-2,4-diones. This strategy employs readily available 5-carbonyl-6-methyluracils, aldehydes, and ammonium iodide under an oxygen atmosphere, affording the target products in good to excellent yields with broad substrate compatibility. The transformation is proposed to proceed via a condensation/cyclization/oxidative dehydrogenation cascade. This method offers notable advantages, such as operational simplicity and environmental benignity, thereby presenting a practical alternative route for the construction of pyrido[4,3-<i>d</i>]pyrimidine-2,4-diones.

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Publication Details

Journal
The Journal of Organic Chemistry
Published
2026-03-23
DOI
https://doi.org/10.1021/acs.joc.5c03158
Primary Topic
Multicomponent Synthesis of Heterocycles
Type
article
Field-Weighted Citation Impact
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article

Three-Component Tandem Annulation for the Synthesis of Pyrido[4,3- d ]pyrimidine-2,4-diones

J. Li, Y. J. Zeng, Xing Liu, Sichen Xu et al.
The Journal of Organic Chemistry
Multicomponent Synthesis of Heterocycles
article

Three-Component Tandem Annulation for the Synthesis of Pyrido[4,3- d ]pyrimidine-2,4-diones

J. Li, Y. J. Zeng, Xing Liu, Sichen Xu, Xue Peng, Tong Chen, Kang Liu, Zhen Wang, Yiming Lei, Jinjin Chen
article en

Abstract

An efficient catalyst- and base-free, three-component tandem annulation has been developed for the synthesis of pyrido[4,3-<i>d</i>]pyrimidine-2,4-diones. This strategy employs readily available 5-carbonyl-6-methyluracils, aldehydes, and ammonium iodide under an oxygen atmosphere, affording the target products in good to excellent yields with broad substrate compatibility. The transformation is proposed to proceed via a condensation/cyclization/oxidative dehydrogenation cascade. This method offers notable advantages, such as operational simplicity and environmental benignity, thereby presenting a practical alternative route for the construction of pyrido[4,3-<i>d</i>]pyrimidine-2,4-diones.

The Journal of Organic Chemistry
Ministry of Education of the People's Republic of China (CN), Qinghai Tibetan Hospital (CN), Hengyang Academy of Agricultural Sciences (CN), University of South China (CN)
Openalex Percentile: Top 11%
Multicomponent Synthesis of Heterocycles
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