Synthesis of Novel 6-Aryloxy-4-chloro-2-phenylpyrimidines as Fungicides and Herbicide Safeners.
Synthesis of Novel 6-Aryloxy-4-chloro-2-phenylpyrimidines as Fungicides and Herbicide Safeners.
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新型杀菌剂和除草剂安全剂 6-芳氧基-4-氯-2-苯基嘧啶的合成
DOI：
10.1021/acsomega.0c03300
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发表时间：
2020-09-22
期刊：
影响因子：
4.1
通讯作者：
Bai L
中科院分区：
文献类型：
--
作者：
Deng X;Zheng W;Jin C;Bai L
氟氯草胺是一种商品化的具有杀菌活性的除草剂安全剂，可作为筛选新型杀菌剂的先导化合物。然而，到目前为止，关于芬氯林或其类似物的杀菌活性构效关系的报道很少。本论文以芬氯林为先导化合物，通过亚结构拼接的方法合成了一系列4-氯-6-取代苯氧基-2-苯基嘧啶类化合物。通过核磁共振氢谱、核磁共振碳谱和高分辨质谱对其结构进行了表征。然后对它们的杀菌和除草安全活性进行了评价。结果表明，化合物11对核盘菌和黄瓜枯萎病菌的杀灭效果最好，优于对照药剂嘧霉胺。此外，化合物3、5和25分别对鲜重、株高和根长表现出良好的安全活性。与芬氯林相比，这种活性显著改善。综上所述，这些发现对于基于氟虫草胺结构的新型杀菌剂和除草剂安全剂的制备是有希望的。
Fenclorim is a commercial herbicide safener with fungicidal activity used for chloroacetanilide herbicides, which might be suitable as a lead compound for screening novel fungicides. However, little has been reported so far on the structure–activity relationship of fungicidal activities of fenclorim or its analogues. Here, a series of 4-chloro-6-substituted phenoxy-2-phenylpyrimidine derivatives was synthesized by a substructure splicing route using fenclorim as a lead compound. The structures of synthesized derivatives were characterized by 1H NMR, 13C NMR, and HRMS. Their fungicidal and herbicide safening activities were then evaluated. The results revealed that compound 11 had the best fungicidal activity against Sclerotinia sclerotiorum and Thanatephorus cucumeris, which was better than that of the control pyrimethanil. Moreover, compounds 3, 5, and 25 exhibited excellent safening activities against fresh weight, plant height, and root length, respectively. Such activities were significantly improved when compared to fenclorim. In summary, these findings look promising for the preparation of new fungicides and herbicide safeners based on the structure of fenclorim.
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影响因子：
4.1
作者：
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通讯作者：
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