1-苯乙酰基-4-芳酰基氨基硫脲的合成及其在碱催化下的环化反应

SYNTHESIS OF 1-PHENYLACETYL-4-AROYLTHIOSEMICAR-BAZIDES AND THEIR CYCLIZATION

1-酰基-4-芳基氨基硫脲类化合物在碱性条件下环化为具有广泛生物活性的3-取代基-4-芳基-1,2,4-三唑啉-5-硫酮的反应报道甚多,但1,4-位都含羰基的酰氨基硫脲在碱性条件下环化反应迄今报道较少。我们曾研究了1-[5-（α-萘）-2H-四唑-2-乙酰基]-4-芳酰基氨基硫脲和1-（α-萘乙酰基）-4-芳酰基氨基硫脲在碱催化下环化为3-取代基-4-芳酰基-1,2,4-三唑啉-5-硫酮的反应,它们在低浓度下均有一定的生物活性。本文研究了1-苯乙酰基-4-芳酰基氨基硫脲1a～m在1mol/L K2CO3溶液催化下的环化反应,得到环化产物3-苄基-4-芳酰基-1,2,

A series of 1-phenylaeetyl-4-aroylthiosemicarbazides (1) were synthesized by the reaction of phenylacetylhydrazine with aroyl isothiocyanates. Some of 3-benzyl-4-aroyl-1,2, 4-triazoline-5-thione (2) were obtained in good yields through the cyclization of 1 in 1mol/LK_2CO_3 solution. The structures of all compounds prepared were characterized by elemental analysis,IR,~1H NMR and MS.The preliminary experiments showed that compounds 1 and 2 possess some inhibiting activity on B. substilis.