【作者】 林奇；

【导师】 魏太保； 张有明；

【作者基本信息】 西北师范大学 ， 有机化学， 2005， 硕士

【摘要】 本论文共分六章 第一章 简要介绍了酰基硫脲衍生物在农药、超分子阴离子识别、超分子自组装等方面的研究情况和应用价值。并对酰基硫脲衍生物的合成方法作了归纳和总结。 第二章 在微波辐射和无溶剂条件下,合成了13种N-苯甲酰基-N′-芳基硫脲,10种N-乙氧羰基-N′-芳基硫脲。结果表明,这种无溶剂微波合成法能大幅度地减少反应时间、提高产率、减少溶剂使用量。因此,这种改进是一种合成此类化合物的简便、高效和环境友好的好方法。另外,通过筛选催化剂,发现TMEDA能很好的提高氯甲酸乙酯中酰氯的反应活性,提高中间体乙氧羰基异硫氰酸酯的产率,从而提高整个反应的产率;用TMEDA催化的方法合成了10种N-乙氧羰基-N′-芳基硫脲及11种芳撑和多亚甲撑二乙氧羰基二硫脲。另外,我们还对化合物BG进行了生物活性实验:通过BG对小麦锈病的田间药效试验,证明了BG对小麦锈病有很高的防治效果（可达84.78%）,可在生产上推广,用于防治小麦锈病;BG对春小麦的增产作用的田间试验表明BG对春小麦有相当的增产作用,是一个值得推广的植物生长调节剂。 第三章 用1,6-二取代酰基二硫脲在DMF中加热回流直接脱H₂S关环的方法合成了11种2,5-二酰胺基-1,3,4-噻二唑,用IR、^H NMR、¹³C NMR和EA等方法对其进行了表征。这种1,6-二取代酰基二硫脲在DMF中加热回流直接脱H₂S关环合成2,5-二酰胺基-1,3,4-噻二唑的方法尚未见文献报道。 第四章 合成了9种含巯基四唑环的酰基硫脲衍生物,并在冷的浓硫酸中对这几种酰基硫脲进行了关环反应,合成了9种2-芳酰氨基-5-（1-苯基-1H-四唑-5-巯基）亚甲基噻二唑。 第五章 用X-射线单晶衍射确定了7个N-乙氧羰基-N′-芳基硫脲、一个2,5-二乙更多还原

【Abstract】 This paper includes six chapters:Chapter One. This chapter is a brief review for the research and application values of acylthioureas in the fields of pesticide, superamolecular anion recognition, superamolecular self-assembly. The synthetic methods of acylthioureas are briefly summarized as well.Chapter Two. Thirteen N-benzoyl-N’-arylthioureas and ten N-ethoxycarbonyl-N’-arylthioureas were synthesized under the microwave irradiation and solvent-free conditions. In conclusion, this method is an efficient and convenient method for the synthesis of N-aryl-N’ -acylthioureas. Moreover, a series of N-aryl-N’-ethoxycarbonyl thioureas and arene （or polymethylene）-bis-ethoxycarbonylthiourea derivatives have been synthesized in good to excellent yields under the TMEDA catalyzed conditions at room temperature. According to the bioactivities tests, the compounds BG have the anti-rust fungus and growth regulating activities of wheat.Chapter Three. A novel method for synthesis 2,5-bis-substituted-1,3,4-thiadiazoles by direct cyclization of 1,6-bis-substituted dithiourea in refluxing DMF solution is presented, eleven 2,5-bis-substituted-l,3,4-thiadiazoles were synthesized using this method. All compounds were characterized by IR, ¹H NMR, ¹3C NMR and EA.Chapter Four. Eleven l-[（l-phenyl-lH-tetrazole-5-yl）thio]acetyl-4-aroylthiosemi-carbazides were synthesized under the condition of phase transfer catalysis in good to excellent yields. By cyclization of these compounds in concentrated H2SO4 at 0℃, corresponding 2-aroylamino-5-[（l-phenyl-lH-tetrazole-5-yl）thio]acetyl methylene-1, 3, 4-thiadiazoles were obtained in high yields. All these products were confirmed by elemental analysis, IR, ’HNMR and ¹3CNMR.Chapter Five. The single crystal structure of seven N-ethoxycarbonyl- N’-arylthioureas,one 2,5-ethoxylcarbonylamide-substituted-l,3,4-tbiadiazole and one N, N’-di（4-bromophenyl）urea were analyzed by X-ray diffraction. There are hydrogen bonding and π staking superamolecular interactions in these crystals. These compounds were self-assembled to one-dimensional linear or two-dimensional netlike superamoleculer structure.Chapter Six. L-aspartic acid zinc was synthesized by a rapid and convenient method in high yield under microwave conditions, and its single crystal structure was analyzed by X-ray diffraction. The structural unit of the title compound is [Zn（L-Asp）（H₂O）₂] H2O, which is a bicyclo-complex forming a spiral linear polymer via coordination bonds. The spiral linear polymers are assembled as a three-dimensional supramolecule by intennolecular hydrogen bonds. The toxicity of the L-aspartic acid zinc is lower than glutamic acid zinc and zinc sulfate.更多还原