共查询到20条相似文献,搜索用时 109 毫秒
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2-巯基苯并噻唑衍生物的合成进展 总被引:1,自引:0,他引:1
2-巯基苯并噻唑具有很好的经济价值.为了增强和完善2-巯基苯并噻唑的应用性能,通过将其作为一种中间体,与油溶性基团的活性元素结合在同一分子内,开发和研究了其一系列新型的具有良好性能的衍生物,可用作配体、染料、硫化促进剂、蛋白质酶抑制剂以及杀菌、除草和抗病毒药物.对通过包括苯环、巯基上的S、杂环上的N等3个位置上的取代或加成来合成这些衍生物的简单可行方法进行了综述. 相似文献
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O,O''''-二烷基-α-(取代苯并噻唑-2-基)氨基-(取代苯基甲基)膦酸酯的合成与抗烟草花叶病毒活性 总被引:1,自引:0,他引:1
采用无溶剂无催化剂合成方法,分别进行了以O,O'-二烷基亚磷酸酯、3,4,5-三甲氧基苯甲醛、2-氨基取代苯并噻唑为原料的类Mannich一锅法合成反应研究,经合成筛选,优选出控制反应温度100℃,无溶剂、无催化剂加热反应120min的合成方法,实验结果表明该方法经济、简便、对环境友好.经元素分析,IR,1HNMR,13CNMR对所合成的化合物进行了结构确认和表征.培养并测定了化合物4a的晶体结构.初步生物活性测试表明,化合物具有一定的抗烟草花叶病毒活性. 相似文献
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为实现多种活性成分的有效叠加和为药物筛选提供先导化合物,以1-苯基-3-甲基-5-氯/苯氧基-4-吡唑甲酸为初始原料,依次合成1-苯基-3-甲基-5-氯/苯氧基-4-吡唑甲酰氯、1-苯基-3-甲基-5-氯/苯氧基-4-吡唑甲酰基异硫氰酸酯,再与取代苯并噻唑肼反应生成了8个未见报道的N-取代苯并噻唑-2-氨基-N'-取代吡唑-4-甲酰基硫脲.采用超声波催化法合成了标题化合物,并与加热回流的常规方法进行了对比.超声波催化法具有操作简单、反应时间短、条件温和、产率高、副反应少等优点,为此类化合物的合成提供了一种有效的新方法.标题化合物经元素分析,IR,1HNMR确证结构. 相似文献
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Mortaza Mirzai 《合成通讯》2013,43(9):1268-1277
A mild, efficient, and solvent-free microwave (MW)–promoted Biginelli reaction for the synthesis of 3,4-dihydropyrimidin-2(1H)-(thio)ones in nitrite ionic liquid (IL-ONO) is described. This ionic liquid is a weak Lewis base catalyst, which can be easily recovered and reused in several runs. The satisfactory results were obtained with good yields and short reaction time, using a simple experimental procedure. 相似文献
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An efficient and green route for the synthesis of dihydropyrimidinones via microwave-assisted Biginelli reaction catalyzed by 3 mol% of heteropolyanion-based ionic liquids under solvent-free conditions has been reported. The practical reaction was found to be compatible with different structurally diverse substrates. Good to excellent yields, short reaction times, and operational simplicity are the main highlights of this protocol. Moreover, the heteropolyanion-based ionic liquids were easily reusable for this Biginelli reaction. 相似文献
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离子液体中乙酸异山梨醇酯的合成 总被引:3,自引:0,他引:3
以1-丁基-3-甲基咪唑六氟磷酸盐离子液体为溶剂,对新一代长效抗心绞痛药物单硝酸异山梨酯中间体异山梨醇进行了萃取分离,避免了使用高真空高温蒸馏;以酸性离子液体N-甲基咪唑硫酸氢盐为溶剂和催化剂,合成了中间体2-乙酸异山梨醇酯,产物结构经红外光谱确证.异山梨醇收率80%,2-乙酸异山梨醇酯收率86%. 相似文献
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以离子液体[Hnmp]HSO4为催化剂, 在无溶剂条件下催化芳香醛、2-氨基苯并噻唑和2-萘酚合成一系列的2 -氨基苯并噻唑-芳甲基-2-萘酚. 该方法条件温和, 反应时间短, 产率高和对环境友好. 此外催化剂可以方便地回收, 且循环使用四次其催化活性并没有显著降低. 目标产物经过了1H NMR, IR, MS和元素分析确证. 相似文献
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The application of microwave techniques for chemical synthesis has attached considerable interests in recent years because of their enhanced selectivity, reduced reaction time ,easier work-up procedure. The synthesis of thiohydantoin derivatives is useful because they display a wide range of biological activities, including anticonvulsant1, antitumor2, antinociceptive3,thyroxine ingibitory properties4, as well as herbicidal and fungicidal reagents5. Recent studies have shown that some used as synthetic precursor of the marine natural product dispacamide6, and some used to synthesis novel optically active poly(amide-imide)s7. Therefore, many methods of synthesis of thiohydantoins have been explored8~10. Generally, these reactions were carried out in solution and using volatile and poisonous solvent, with long reaction time.In order to overcome the disadvantages discussed above, avoid the use of a solvent and synthesize these valuable compounds rapidly and efficiently, we investigated a new way---solvent-free synthesis using a microwave oven.In this paper, a new and rapid solvent-free synthesis of thiohydantoins with microwave activation was studied. It was found that the addition reaction of aryl isothiocyanates and amino acid in the presence of sodium hydroxide and the cyclizative condensation of adduct in the presence of sodium hydrogen sulphate in a microwave oven takes place quickly.By this new method, twelve thiohydantoins have been synthesized in excellent yield(83~91%).This method has significant advantages such as operational simplicity, shorter reaction time, higher yields and environmental acceptability. The structures of the products were characterized by IR, MS,1H NMR, 13C NMR and elemental analysis. And more detailed work about the application of the thiohydantoins in analytical chemistry and physiological activity is in progress in our laboratory. 相似文献