新型2,2-二氟-1,3-苯并二茂衍生物的合成与杀菌活性  

Synthesis and Fungicidal Activity of Novel 2,2-Difluoro-1,3-benzodioxole Derivatives

作　　者：王威[1] 黄晓瑛[1] 王列平[1] 刘康云[1] 郑晓蕊[1] 贺红武[2] WANG Wei;HUANG Xiao-ying;WANG Lie-ping;LIU Kang-yun;ZHENG Xiao-rui;HE Hong-wu(State Key Laboratory of Fluorine&Nitrogen Chemicals,Xi'an Moderm Chemistry Research Institute,Xi'an 710065,China;Key Laboratory of Pesticide&Chemical Biology of Ministry of Education,College of Chemistry,Central China Normal University,Wuhan 430079,China)

机构地区：[1]西安近代化学研究所氟氮化工资源高效开发与利用国家重点实验室,西安710065 [2]华中师范大学化学学院农药与化学生物学教育部重点实验室,武汉430079

出　　处：《农药》2021年第8期563-566,590,共5页Agrochemicals

基　　金：西安市科技计划项目(2020KJC0145)。

摘　　要：[目的]为了获得具有杀菌活性的新型2,2-二氟-1,3-苯并二茂衍生物。[方法]基于活性亚结构拼接原理,将1,3,4-二唑与2,2-二氟-1,3-苯并二茂结合。[结果]合成了9个结构新颖的2,2-二氟-1,3-苯并二茂类衍生物,并对其进行了杀菌活性测试,其中化合物I-1在100 mg/L下对苹果树腐烂病菌和番茄灰霉病菌的抑制活性为100%,化合物6在100 mg/L下对苹果树腐烂病菌、小麦赤霉病菌和番茄灰霉病菌的抑制活性为100%。[结论]目标化合物I-1和6具有一定的杀菌活性,值得进一步研究。[Aims] This study aims to find novel 2,2-difluoro-1,3-benzodioxole derivatives with higher fungicidal activity. [Methods] Based on the fragment combination, 1,3,4-oxadiazole and 2,2-difluoro-1,3-benzodioxole groups were combined. [Results] Nine novel 2,2-difluoro-1,3-benzodioxole derivatives were synthesized, and their fungicidal activities were evaluated. Compound I-1 showed 100% inhibiton effect against Valsa mali and Botrytis cinerea at 100 mg/L,and compound 6 displayed 100% inhibiton effect against V. mali, Fusarium graminearum and B. cinerea at 100 mg/L.[Conclusions] The target compounds I-1 and 6 show good fungicidal activities, which could be modified for further study.

关 键 词：2 2-二氟-1 3-苯并二茂 1 3 4-二唑 合成 杀菌活性 

分 类 号：TQ460.3[化学工程—制药化工]