Diiodo-acetamide derivs. - for use as antibacterials, antimycotics, anthelmintics and animal feed additives

摘要

Prepn. of new diiodoacetamide derivs. of formula (I):- R1-NH-CO-CHI2 (where R1 is lower alkyl, cycloalkyl, naphthyl, or phenyl opt. substd. by F, Dl, Br, I, lower alkoxy, lower alkyl, lower alkoxycarbonyl, CF3, No2 or sec. amino) comprises treating a 2-carbamoyl-1,3-cyclohexanedione of formula (II) or an acetoacetamide deriv. of formula (III) with an aq. iodide-contg. iodine soln. in an alkaline medium;- (where R1' is a defined for R1 but not alkyl or cycloalkyl; ring A is opt. substd. in the 4,5 and 6 posns.). Cpds. (I) are useful as (a) antibacterial agents, e.g. with MIC values of 0.6-50 mug/ml; (b) antimycotic agents, e.g. with MIC values of 0.08-50 mug/ml against Trichophyton quinckeaneum and Aspergillus fumigatus; (c) anthelmintics, esp. active and against cestodes; and (d) animal feed additives for improving feed utilisation in ruminants. In an example, 2,2-diiodo-m-chloracetanilide is prepd from 2-(m-chlorophenylcarbamoyl)-1,3-cyclohexanedione.