Synthesis and Bioactivity of 2-(Pyridyl-2-formyl)pyrimidine Derivatives

doi:10.6023/cjoc201412034

Chin. J. Org. Chem. ›› 2015, Vol. 35 ›› Issue (6): 1342-1347.DOI: 10.6023/cjoc201412034 Previous Articles Next Articles

Notes

2-(吡啶-2-甲酰基)嘧啶类化合物的合成与生物活性研究

吕强^a,b, 芦昕婷^b, 张基胜^b, 张志国^b, 朱为宏^a, 杜葩^c, 吕龙^b

a 华东理工大学化学与分子工程学院上海 200237;
b 中国科学院上海有机化学研究所有机氟化学重点实验室上海 200032;
c 上海应用技术学院化学与环境工程学院上海201418

收稿日期:2014-12-19 修回日期:2015-02-05 发布日期:2015-02-10
通讯作者: 杜葩 E-mail:dupa@sit.edu.cn
基金资助:
"十二五"国家科技支撑计划(No. 2011BAE06B02)资助项目.

Synthesis and Bioactivity of 2-(Pyridyl-2-formyl)pyrimidine Derivatives

Lü Qiang^a,b, Lu Xinting^b, Zhang Jisheng^b, Zhang Zhiguo^b, Zhu Weihong^a, Du Pa^c, Lü Long^b

a School of Chemistry and Molecular Engineering, East China University of Science and Technology, Shanghai 200237;
b Key laboratory of Organofluorine Chemistry, Shanghai Institute of Organic Chemistry, Chinese Academy of Science, Shanghai 200032;
c School of Chemical and Environmental Engineering, Shanghai Institute of Technology, Shanghai 201418

Received:2014-12-19 Revised:2015-02-05 Published:2015-02-10
Supported by:
Project supported by the National Key Technologies R&D Program (No. 2011BAE06B02)

1. Synthesis and Bioactivity of 2-(Pyridyl-2-formyl)pyrimidine Derivatives.PDF(654KB)

Abstract

Based on the structural optimization of 2-benzoyl pyrimidine derivatives, eight 2-(pyridyl-2-formyl)pyrimidine derivatives have been specifically designed and synthesized for evaluation of their interior fungicidal activities. 2-(Pyridyl-2-formyl)pyrimidine derivatives show excellent activity against cucumber downy mildew and cucumber powdery mildew. Among them, 2-chloro-N-{[2-(4,6-dimethoxypyrimidine-2-carbonyl)pyridin-3-yl]oxy}-N-methylbenzamide (6b) exhibits comparable protective and curative activity against cucumber powdery mildew to reference Metrafenone. EC₅₀ and EC₉₀ of the protective activity are 0.69 and 2.89 mg/L, respectively, and those of curative activity are 0.13 and 1.6 mg/L. 6b also shows excellent upward translocation in plants and rainfast performance. Especially, its persistent efficacy period of the protective activity against cucumber powdery mildew can last 15～20 d.

Key words: 2-(pyridyl-2-formyl)pyrimidine, synthesis, fungicidal activity

Cite this article

Lü Qiang, Lu Xinting, Zhang Jisheng, Zhang Zhiguo, Zhu Weihong, Du Pa, Lü Long. Synthesis and Bioactivity of 2-(Pyridyl-2-formyl)pyrimidine Derivatives[J]. Chin. J. Org. Chem., 2015, 35(6): 1342-1347.

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2-(吡啶-2-甲酰基)嘧啶类化合物的合成与生物活性研究

Synthesis and Bioactivity of 2-(Pyridyl-2-formyl)pyrimidine Derivatives

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