| 摘要 |
<p>Prepn. nitroimidazole derivs. of formula (I) and their acceptable acid addn. salts comprises first reacting 2-nitroimidazole (II) with a haloalkanol of formula Hal.A.OH (III). The product is reacted with 2,2,2-trichloroethyl chloroformate (IV) and then with an amine, HX, and opt. (I) formed converted to a salt. (A is 2-6C polymethylene chain. X is NH2 opt. substd. by 1 or 2 1-7C alkyl, or by 1 1-7C hydroxyalkyl, cycloalkyl, heteroarylalkyl, aralkyl or aryl, or X is -N Z where Z is 1-7C alkylene opt. substd. by NH,O or N(1-7C alkyl). (I) are antiprotozoals and antibacterials, esp. useful for control of protozoa such as Trichomonas vaginalis, T. foetus or Endamoeba histolytica. They are presented in usual formulations for an oral dose of 5-50mg/kg. In an example 2-(2-nitro-1-imidazoyl)ethyl-N-furfuryl carbamate was prepd. from (II) by sequential reaction with 2-bromoethanol, (IV) and furfurylamine.</p> |
