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微波辐射下合成1-(2-三氟甲基苯并咪唑-1-乙酰基)-4-芳酰基氨基硫脲

Synthesis of 1-(2-Trifluoromethylbenzimidazol-1-acetyl)-4-Aroylthiosemicarbazide under Microwave Irradiation
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摘要 分别使用微波辐射法和常规加热回流方法,采用活性基团亚结构连接法,由1-肼羰亚甲基-2-三氟甲基苯并咪唑与芳酰基异硫氰酸酯(1a~1k)反应,合成了一系列未见文献报道的1-(2-三氟甲基苯并咪唑-1-乙酰基)-4-芳酰基氨基硫脲(2a~2k)。与常规法相比,微波辐射法反应过程简单、反应时间较短、产率较高、副反应少、产物易纯化。其结构由元素分析、IR、1H NMR分析得到确证。生物活性初步实验结果表明,在初始质量浓度为200 mg/L条件下,只有化合物2a稍具抗HIV-1逆转录酶活性。 A series of novel 1 - ( 2-trifluoromethylbenzimidazol-1-acetyl ) -4-aroylthios-emicarbazides (2a - 2k) was synthesized by the reaction of 1-hydrazinocarbonylmethyt-2-trifluoromethylbenzimidazole with each of aroylisothiocyanates(la -1k) under microwave irradiation and classical heating conditions. Compared to classical heating method, microwave irradiation has many advantages in the organic synthesis process, such as simple operation, short reaction time, high yields, less side reactions and easy purification of products. The structures of these compounds were confirmed by elemental analysis, IR, and ^1H NMR. The preliminary biological activities of the target compounds were tested, and the result showed that only compound 2a had low anti-HIV-1 reverse transeriptase aetivity.
出处 《应用化学》 CAS CSCD 北大核心 2009年第1期59-62,共4页 Chinese Journal of Applied Chemistry
基金 国家自然科学基金(20662009) 教育部博士点专项基金(20050755003)资助项目
关键词 微波辐射 苯并咪唑 芳酰基氨基硫脲 合成 microwave irradiation,benzimidazole,aroyhhiosemicarbazide, synthesis
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