Studies On Synthetic Methods,Bioactivities And Superamolecular Crystal Structures Of Bioactive Compounds

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 Ï€ 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.