5-(4-吡啶基)-2-芳酰氨基-1,3,4-噻二唑的合成与环化反应

Synthesis of 5-(4-Pyridyl)-2-Aroylamino-1,3,4-Thiadiazoles and Cyclization Reaction

由异烟肼与芳酰异硫氰酸酯在无水CaCl_2处理过的乙腈溶剂中亲核加成,制得一系列1-(4-吡啶酰基)-4-芳酰氨基硫脲衍生物Ⅰ。Ⅰ在酸性溶液中环化脱水为5-(4-吡啶基)-2-芳酰氨基-1,3,4-噻二唑Ⅱ。所有产物Ⅱ的结构均经元素分析、IR、~1H-NMR和MS鉴定,部分化合物对金色葡萄球菌和大肠杆菌有抑制作用。

A series of new 1- ( 4-pyridylcarbonyl ) -4-aroylthiosemicarba-zides (l) were synthesized by condensation of aroyliso-thiocyanate with isonicotinyl hydrazine in unhydrous acetonitrile. Some of 5-(4-pyridyl)-2-aroylamino-1,3,4-thiadiazoles (II) were obtained in good yields (70.1-99.0%) by cyclization of compounds(l) in acid solution, The structures of all the synthesized compounds were characterized by elemental analysis, IR, 1H-NMR and MS. Some of the( II )compounds exhibited strong inhibiting effect on StaphylocOcus Aureus and Escherichia Coli.