(N)-Methoxy-carbonyl ring-substd. phenyl-guanidine cpds. - useful as anthelmintics and suitable for parenteral administration to large animals such as cattle and horses

摘要

Guanidine derivs. of formula (I) and salts with (in)organic acids are new. In the formula, X is O, S, SO, SO2 or CO, or 4- or 5-position of ring A. R is H, halo, 1-4C alkoxy or CF3. R1 is H or opt. substd. alkyl, alkoxy, alkoxyalkyl or aralkyl. R2 is H, alkyl, cycloalkyl, cycloalkylalkyl or aralkyl. (I) are prepd. e.g. by reacting the appropriate aniline with R3S.C(NHR2)=NCOOCH3 (R3 is 1-4C alkyl). (I) are anthelmintics. They can be given orally or, unlike other phenylguanidines, parenterally as aq. solns. They are esp. useful for mass treatment of large animals such as cattle and horses. In an example, N-(2-methoxy-acetamido-4-phenylthiophenyl)-N1-methoxycarbonyl-gua- nanilide was prepd. from 2-amino-5-phenylthio-methoxyacetanilide and N-methoxycarbonyl-S-methyl-isothiourea.