In order to obtain novel botanical fungicides, three series of novel 6-substituted n-butyphthalide derivatives have been designed and synthesized via nucleophilic addition, reduction, nitrification, amination, sulfonation, Sandmeyer and Suzuki reaction. The mycelium growth rate method was used to evaluate the inhibition activity against eight phytopathogenic fungi in vitro. Preliminary bioassay tests showed that compounds 6f, 6n, 6p, 6r and 7a exhibited better activity for some fungi at 50 μg/mL than the positive drug hymexazol and lead compound n-butyphthalide (NBP). The preliminary structure-activity relationships indicated that the antifungal activity is significantly affected by the substituents on the benzene ring.

中文翻译：

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作为有前途的植物杀菌剂的新型正丁苯酞衍生物的设计与合成

为获得新型植物杀菌剂，通过亲核加成、还原、硝化、胺化、磺化、Sandmeyer和Suzuki反应，设计并合成了三个系列的新型6-取代正丁苯酞衍生物。采用菌丝体生长速率法评价体外对八种植物病原真菌的抑制活性。初步生物测定测试表明，化合物 6f、6n、6p、6r 和 7a 在 50 μg/mL 时对某些真菌表现出比阳性药物 hymexazol 和先导化合物正丁苯酞（NBP）更好的活性。初步的构效关系表明苯环上的取代基显着影响抗真菌活性。