摘要
以乙酰基香豆素经四丁基三溴化铵溴化作用生成的3-溴乙酰基香豆素为起始原料、PEG-400为溶剂,设置超声功率为40 k Hz、辐射时间为20-40 min,通过与芳基硫脲的缩合环化反应制备标题化合物,收率为81.6%-93.0%,其结构经IR、^1HNMR、^13CNMR、MS和元素分析等手段加以确证。实验结果表明,部分目标化合物对金黄色葡萄球菌、枯草杆菌和大肠杆菌都有不同程度的抑制作用。所使用的反应媒介对环境友好,可以回收并多次使用。
In this work,3-（ 2-bromoacetyl）-2 H-chromen-2-ones prepared from 3-acetyl coumarins with tetrabutylammonium tribromide on bromination were used as the raw material.An efficient approach toward the synthesis of 4-（ coumarin-3-yl）-2-arylaminothiazoles was carried out by the reaction of the starting compounds with certain phenyl thioureas in presence of PEG-400 under ultrasound irradiation at a frequency of 40 kHz in 20 - 40 min,with a yield of 81. 6% - 93. 0%.The structures of target compounds were confirmed by IR,^1HNMR,^13CNMR,MS and elemental analysis.Preliminary bioassay results showed that some of them have certain antibacterial activities against Staphylococcus Aureus,Bacillus Subtilis and Escherichia Coli. This method is operationally simple and environmentally benign and the solvent could be reused for several times.
作者
雷英杰
吴新世
张国春
LEI Ying-jie;WU Xin-shi;ZHANG Guo-chun(Tianjin Key Laboratory of Organic Solar Cells and Photochemical Conversion,School of Chemistry ＆ Chemical Engineering, Tianjin University of Technology, Tianjin 300384, China;Shanxi Key Laboratory of Comprehensive Utilization of Tailings Resources, Shangluo University, Shangluo 726000, China)
出处
《化学试剂》
CAS
北大核心
2018年第6期518-522,588,共6页
Chemical Reagents
基金
天津市科技特派员项目(16JCTPJC49800)
