抗滴虫药1-(2-乙基磺酰基乙基)-2-甲基-5-硝基咪唑的合成

Synthesis of 1 - (2 - ethylsulfonylethyl) - 2 - Methyl-5-Nitroimidazole as Antitrichomonal Drug

文中报道了一种抗滴虫药物1-(2-乙基磺酰基乙基)-2-甲基-5-硝基咪唑[即替硝唑,(1)]的简便合成方法。该方法以2-甲基-5-硝基味唑(5)为原料,(5)与β-羟基乙基乙硫醚(4)在酸催化下缩合生成1-(2-乙硫基乙基)-2-甲基-5-硝基味唑(6),过量的2-甲基-5-硝基咪唑可回收利用,(6)经过氧化氢氧化生成替硝唑。

1 - (2 - ethy sulfonylethyl) - 2 - methyl - 5 - nitroimidazole [ tinidazole, (1) ] , as a highly potent antitrichomonal drug, has been synthesized by a facile method. Acid - catalysed condensation of 2 - methyl - 5 - nitroimidazole(5) with ethyl(2 - hydroxylethyl) sulfide(4) led to 1 - (2 - ethyl -thioethyl) - 2 - methyl - 5 - nitroimidazole(6) , and exess(5) can be recovered. (6)was oxidized to tini-dazole(1) by H2O2 in the presence of ammonium molybdenate in a good yield.