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2-苯甲酰基嘧啶类化合物的合成与生物活性
Alternative TitleSynthesis and Bioactivity of 2-Benzoyl Pyrimidine Derivatives
吕强1; 芦昕婷1; 戴明1; 刘世梦1; 朱为宏1; 杜葩1; 吕龙1
2015
Source Publication有机化学
Volume35Issue:6Pages:1260-1269
Other Abstract2-Benzoyl pyrimidine as a secondary leading structure is developed by twice optimization of 2-pyrimidinoxy-N-aryl benzylamine. Based on this structure, thirty six 2-benzoyl pyrimidine derivatives have been designed and synthesized. All compounds are determined by H-1 NMR, C-13 NMR. and HRMS. Their interior fungicidal activities show that R-1 substituent prefers phenyl or heterocyclic group with 2-halo or 2-alkyl group. When introducing fluoride to 6-position on benzene ring, the fungicidal activity is maintained at a similar level. 4,6-Dimethoxy group on pyrimidine ring was recognized as a best substituent by far. The activity is seriously decreased when methyl group is fixed on 5-position of pyrimidine. Even the fungicidal activities become completely disappeared when the ketone group is reduced to hydroxyl group. Among them, three compounds 2,3-dichloro-N-(2-(4,6-dimethoxypyrimidine-2-carbonyl)phenoxy)-N-methylbenzamide (4AHI), 2,5-dichloro-N-(2-(4,6-dimethoxypyrimidine-2-carbonyl)phenoxy)-N-methylbenzamide (4AHn) and N-(2-(4,6-dimethoxypyrimidine-2-carbonyl)-3-fluorophenoxy)-N,2-dimethylbenzamide (4AFd) exhibit comparable fungicidal activity against cucumber powdery mildew to the reference metrafenone.
Subtype论文
Subject Area有机化学
DOI10.6023/cjoc201412032
URL查看原文
Indexed BySCI
Language中文
WOS IDWOS:000359274400007
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Document Type期刊论文
Identifierhttp://ir.sioc.ac.cn/handle/331003/39740
Collection中科院有机氟化学重点实验室
Corresponding Author杜葩
Affiliation1.华东理工大学
2.中科院上海有机化学研究所, 有机氟化学重点实验室
3.上海应用技术学院
Recommended Citation
GB/T 7714
吕强,芦昕婷,戴明,等. 2-苯甲酰基嘧啶类化合物的合成与生物活性[J]. 有机化学,2015,35(6):1260-1269.
APA 吕强.,芦昕婷.,戴明.,刘世梦.,朱为宏.,...&吕龙.(2015).2-苯甲酰基嘧啶类化合物的合成与生物活性.有机化学,35(6),1260-1269.
MLA 吕强,et al."2-苯甲酰基嘧啶类化合物的合成与生物活性".有机化学 35.6(2015):1260-1269.
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