In the course of discovering novel fungicidal lead compounds with high activity and safety, 13 new difluoromethyl substituted carboxamide derivatives were designed and synthesized according to the principle of bioactive substructure combination. Their structures were confirmed by 1 H NMR, MS and HRMS. The fungicidal activities of these compounds were evaluated. Preliminary bioassay showed that most of the title compounds showed good fungicidal activity at 200 mg/L.
To find new fungicidal lead compounds with high bioactivity, novel lead compounds were designed by active group splicing. The synthetic routes are as follows: 6-chloro-2-(2,6-difluorophenyl)quinoline-4-carbonyl chloride (7) was synthesized using 5-chlorine isatin (4) and 2,6-difluoro acetophenone (5) as raw materials by cyclization, acyl chlorination and other step reactions. Then 13 novel title compounds were synthesized by acylation of 6-chloro-2-(2,6-difluorophenyl)-quinoline-4-carbonyl chloride (7) with substituted anilines (8). The structures of the compounds were confirmed by HRMS and 1 H NMR. The preliminary fungicidal activity showed that all the compounds exhibit fungicidal activity against Gaeumannomyces graminis and Fusahum graminearum sehw, Rhizoctonia cerealis and Pyricularia grisea at concentration of 50 mg/L, part of compounds against Gaeumannomyces graminis were more than 90% at concentration of 50 mg/L.
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