6-溴-4-烃硫基喹唑啉类化合物的合成及抑菌活性研究有机化学.pdfVIP

2008 年第 28 卷 有 机 化 学 Vol. 28, 2008 第 7 期, 1268～1272 Chinese Journal of Organic Chemistry No. 7, 1268～1272 ·研究简报· 6-溴-4-烃硫基喹唑啉类化合物的合成及抑菌活性研究 马 耀 刘 芳 严 凯 宋宝安* 杨 松 胡德禹 金林红 薛 伟 (贵州大学精细化工研究开发中心 教育部绿色农药和生物工程重点实验 贵阳 550025) 摘要 以 6-溴-4-巯基喹唑啉和卤代烃为原料, 用相转移催化法合成了 10 个新的 6-溴-4-烃硫基取代喹唑啉类化合物. 化合物经 1H NMR, 13C NMR, IR 及元素分析证明其结构. 初步生物活性试验结果表明, 在 50 mg•L－1 浓度下, 化合物 6g 对小麦赤霉病菌、辣椒枯萎菌、苹果腐烂菌抑制率分别为 63.8%, 51.9%, 55.1%, 与对照药剂恶霉灵抑制活性相当. 关键词 喹唑啉; 溴; 硫醚; 抑菌活性 Synthesis and Antifungal Bioactivity of 6-Bromo-4-alkylthio- quinazoline Derivatives MA, Yao LIU, Fang YAN, Kai SONG, Bao-An* YANG, Song HU, De-Yu JIN, Lin-Hong XUE, Wei (Key Laboratory of Green Pesticide and Bioengineering, Ministry of Education , Research and Development Center for Fine Chemicals, Guizhou University, Guiyang 550025) Abstract Ten new 6-bromo-4-alkylthioquinazoline compounds were synthesized by the reaction of 6-bromo-4-thiolquinazoline with alkylhalide under the conditions of phase-transfer catalysis. The structures 1 13 of the new compounds were characterized by H NMR, C NMR, IR spectra and elemental analyses. Bioac- tivity of the new compounds was tested. The preliminary bioassay showed that compound 6g had certain an- tifungal activities against Fusarium graminearum, Cytospora mandshurica and Fusarium oxysporum with