| 3-杂环基硫取代-1,3,4,5-四氢-2-氧代-苯并氮杂衍生物的合成 |
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| 引用本文： | 邱早早,张欢欢,惠新平,许鹏飞,王勤,杜宇平,杨洋.3-杂环基硫取代-1,3,4,5-四氢-2-氧代-苯并氮杂衍生物的合成[J].有机化学,2007,27(5). |
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| 作者姓名： | 邱早早 张欢欢 惠新平 许鹏飞 王勤 杜宇平 杨洋 |
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| 作者单位： | 1. 兰州大学化学化工学院,功能有机分子化学国家重点实验室,兰州,730000
2. 兰州大学生命科学学院,兰州,730000 |
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| 基金项目： | 国家自然科学基金，教育部跨世纪优秀人才培养计划，高等学校博士学科点专项科研项目 |
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| 摘 要： | 以芳酰肼为原料,合成了一系列3-巯基-5-芳基-1,2,4-三唑、2-巯基-5-芳基-1,3,4-噁二唑和2-巯基-5-芳基-1,3,4-噻二唑,并通过硫原子对3-溴-2-氧代-苯并氮杂3-位上的亲核取代反应将杂环化合物引入了苯并氮杂的结构当中,合成了32个新的苯并氮杂杂环衍生物.为提高其在有机溶剂中的溶解性,在苯并氮杂的N原子上引入乙酸乙酯和乙酸叔丁酯基取代基,合成了36个新衍生物.所有化合物经质谱、核磁共振谱及元素分析确证了结构并初步测定了抗菌活性.
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| 关 键 词： | 苯并氮杂 杂环化合物 亲核取代反应 抗菌活性 |
Synthesis of 3-Thioheterocycloyl-1,3,4,5-tetrahdro-2-oxo-1H-benazepine |
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| QIU Zao-Zao,ZHANG Huan-Huan,HUI Xin-Ping,XU Peng-Fei,WANG Qin,DU Yu-Ping,YANG Yang.Synthesis of 3-Thioheterocycloyl-1,3,4,5-tetrahdro-2-oxo-1H-benazepine[J].Chinese Journal of Organic Chemistry,2007,27(5). |
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| Authors: | QIU Zao-Zao ZHANG Huan-Huan HUI Xin-Ping XU Peng-Fei WANG Qin DU Yu-Ping YANG Yang |
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| Institution: | QIU,Zao-Zaoa ZHANG,Huan-Huana HUI,Xin-Pinga XU,Peng-Fei*,a WANG,Qinb DU,Yu-Pingb YANG,Yangb |
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| Abstract: | 3-Thiol-1,2,4-triazole, 2-thiol-1,3,4-oxadiazole and 2-thiol-1,3,4-thiadiazole compounds were synthesized from hydrazides through different ways. By the nucleophilic substitution of S for Br on 3-bromo-1,3,4,5-tetrahydro-2-oxo-1H-benazepine, 32 derivatives of tetrahydro-2-oxo-1H-benazepine were synthesized. In order to improve dissolving ability in organic solvents, other 36 derivatives, which have a substituent of acetate on the 1-N position of benazepine, were also prepared. The structures of these com-pounds were confirmed by MS, 1H and 13C NMR spectra and elemental analysis. The primary antibacterial activity test indicated that some of the compounds were effective against Bacillus subtilis, Staphylococcus aureus, Escherichia coli, Streptococcus and Candida albicans. |
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| Keywords: | benazepine heterocyclic compound nucleophilic substitution antibacterial activity |
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