1－［5－（3－甲基苯基）－2H－四唑－2－乙酰基］－4－芳酰基氨基硫脲及其环化反应

SYNTHESIS OF 1-[5-(3-METHYLPHENYL)-2H-TETRAZOL-2-ACETYL]-4-AROYLTHIOSEMICARBAZIDES STUDIES OF THEIR CYCLIZATION REACTION

通过５－（３－甲基苯基）－２Ｈ四唑－２－乙酰肼与芳酰基异硫氰酸酯在无水无腈中缩合制得了一系列新的１－［５－（３－甲基苯基）－２Ｈ－四唑－２－乙酰基）－４－芳酰氨基硫脲１＿（ａ～ｋ），１＿（ａ～ｋ），在浓硫酸作用下，得到了新的２－芳酰氨基－５－［５－（３－甲基苯基）－２Ｈ四唑－２－亚甲基］－１，３，４－噻二唑２＿（ａ～ｋ）．１＿（ａ～ｋ）和２＿（ａ～ｋ）在１．５×１０￣（－４）ｍｏｌ·Ｌ￣（－１）浓度下对大肠杆菌和枯草芽孢杆菌的繁殖均有一定的抑制作用。

A series of new 1-[5-(3-methylphenyl)-2H- tetrazol- 2-ylacetyl]-4-aroylthicoemicarbazides 1_(a～k)were synthesized by the condensation of aroylisothiocyanates with 5-(3-methylphenyl)-2H-tetrazol-2-acetylhyclrazine in anhydrous acetonitrile. some new 2-aroylamino-5-[5-(3-methylpheny)-2H-tetra-zol-2-ylmethene]-1-3,4-thiadiazole 2_(a～k)have been synthesized from compeunds 1_(a～k) by treatmentwith conc, sulphuric acid.When tested on Escherichia coli and Bacillus substilis at 1.5×10￣(-4) mol/L,the compounds have some inhibiting activities