| 摘要 |
<p>1-Amidino-3-phenyl-urea derivs. are cpds. of formula (I) and their non-toxic acid addition salts are new. In formula (I) R2-6 are H, halogen, lower alkyl, halo-(lower alkyl), NO2, lower alkoxy, OH, aryl-(lower alkoxy), acyloxy, CN, halo-(lower alkoxy) or lower alkylsulphonyl; R is H or lower alkyl; R' and R" are H, alkyl, cycloalkyl or aralkyl, or NR'R" is a 5- to 7-membered ring contg. up to 2 hetero atoms, namely N, O or S; and R7 is H or lower alkyl; provided that >1 of R, R' and R" is other than H. (I) are effective agents against diarrhoea, but lack the addictive side-effects of conventional anti-diarrhoeals. Specific cpd. is 1-amidino-3-(2,6-dimethylphenyl)urea. In an example, this is prepd. by refluxing 2,6-dimethylaniline with COCl2 in benzene to give 2,6-dimethylphenyl isocyanate and reacting this with guanidine carbonate in tetra-hydrofuran in the presence of KOH.</p> |
