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

作　　者：吕强[1,2] 芦昕婷[2] 张基胜[2] 张志国[2] 朱为宏[1] 杜葩[3] 吕龙[2] 

机构地区：[1]华东理工大学化学与分子工程学院,上海200237 [2]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 [3]上海应用技术学院化学与环境工程学院,上海201418

出　　处：《有机化学》2015年第6期1342-1347,共6页Chinese Journal of Organic Chemistry

基　　金："十二五"国家科技支撑计划(No.2011BAE06B02)资助项目~~

摘　　要：在2-苯甲酰基嘧啶类化合物结构优化结果基础上,定向设计合成了8个2-（吡啶-2-甲酰基）嘧啶类化合物,并对其进行了室内杀菌活性测定,结果表明这类化合物对黄瓜白粉病和黄瓜霜霉病有很好的防效.对高活性化合物6b深入筛选结果表明：6b对黄瓜白粉病有较好的预防和治疗活性,预防活性的EC50和EC90值分别为0.69和2.89 mg/L,治疗活性EC50和EC90值分别为0.13和1.6 mg/L,与对照药剂苯菌酮相当.2-氯-N-{[2-（4,6-二甲氧基嘧啶-2-甲酰基）吡啶-3-基]氧基}-N-甲基苯甲酰胺（6b）具有向上传导活性和较好的耐雨淋作用,持效期为15~20 d.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.

关 键 词：2-(吡啶-2-甲酰基)嘧啶 合成 杀菌活性 

分 类 号：O626[理学—有机化学] TQ450.1[理学—化学]