3-巯基-1,2,4-三氮唑类衍生物的合成研究

Research on Synthesis of 1H-1,2,4-Triazole-3-Thiols Derivatives

研究了以酰氯及硫代氨基脲为原料,在吡啶的作用下,经酰化和环合得到3-巯基-1,2,4-三氮唑类衍生物,收率为85%～90%;以异硫氰酸酯及酰肼为原料,四氢呋喃为反应介质,经酰化和环合2步得到3-巯基-1,2,4-三氮唑类衍生物,收率为90%～92%。2条工艺路线,具有反应收率高、时间短、条件温和等特点,产业化应用价值大。

1H-1,2,4-Triazolo-3-thiols derivatives were important pharmaceutical intermediates with broad spectrum of bioactivities.Two improved processes for the preparation of 1H-1,2,4-triazolo-3-thiols derivatives were researched.The first route included the acylation of acyl chloride and thiosemicarbazide in the presence of pyridine,then cyclization with a totoal yield of 85%~90%.The other route included the acylation of isosulfocyanide and hydrazide using THF as solvent,then cyclization with a totoal yield of 90%~ 92%.The two processes had advantages including high yield,short reaction time and mild reaction conditions,which leaded to high application value in industrialization.