摘要
以2,4-二甲基噻唑-5-甲酸为原料,经酰化与取代苯并嗪酮胺反应,合成了16个未见文献报道的N-(7-氟-2,4-三取代-3-氧-3,4-二氢-2H-苯并[b][1,4]噁嗪-6-基)-2,4-二甲基-5-噻唑酰胺类化合物(3),所有目标化合物结构均通过1HNMR、IR和LC/MS确证。初步生物活性测试表明该类化合物具有不同程度的杀菌活性。在质量浓度500mg/L下,化合物3f、3e、3g对小麦白粉病菌抑制率分别达85.0%、95.0%、100.0%,表现出较好的抑制活性;化合物3i对油菜菌核病菌抑制率达82.2%。
2,4-Dimethylthiazole-5-carboxylic acid as the starting substrate, acylated with substituted benzoxzinonyl amine to synthesize sixteen novel N-（7-fluoro-2,4-substituted-3-oxo-3,4-dihydro-2H-benzo[b][1,4]oxazin-6-yl）- 2,4-dimethylthiazole-5-carboxamides（3）. Their structures were confirmed by IR, ^1H NMR, LC/MS. Preliminary bioassay showed that these novel compounds have different degree fungicidal activities, for example, compounds 3f, 3e and 3g possess 80, 95.5 and 100% fungicidal control at the concentration of 500 mg/L against Erysiphe graminis, respectively, and compound 3i shows 82.2% fungicidal activity against Sclerotonia sclerotiorum.
出处
《农药》
CAS
北大核心
2009年第1期19-22,46,共5页
Agrochemicals
基金
国家自然科学基金资助项目(20872033)
湖南省自然科学基金资助项目(07JJ1003)
晓庄学院化学生物学及中药分析教育部重点实验实验室开放基金资助项目(KLCBTCMR2008-14)
关键词
苯并噁嗪
噻唑酰胺
合成
杀菌活性
benzoxazine
thiazolamide
synthesis
fungicidal activity
