| 摘要 |
The invention comprises imidazoles of the general formula <FORM:1026409/C2/1> and the non-toxic salts with inorganic or organic acids, wherein R is -OH or -SH; R1 is H, methyl, carboxy or carbalboxy; R2 is C1- 10-alkyl, C2- 6-alkenyl, C3- 7-cycloalkyl, o , o -dialkoxyalkyl (at most 6C), dialkylamino alkyl (in all at most 10C and wherein the two alkyl groups together with N can form a 5-7 membered ring), phenyl, phenylalkyl (at most 4C in the alkylene residue) the phenyl group being optionally substituted by halogen, OH, CN, NO2, CF3, CO2H, CH3CO2, CO2C2H5, alkylthio, alkanoyl (at most 4C) or 1-3 alkyl or alkoxy groups (at most 4C in each radical) and the preparation thereof (wherein R is OH) by reacting HCHO, and amine R2NH2 and a ketone <FORM:1026409/C2/2> wherein R11 is methyl or carbalkoxy in a polar solvent, or first forming the Schiffs base and reacting this with III; or (wherein R is SH) by reacting HCHO, R2NH2 and III in a polar solvent, with a reactant which gives off the hydrosulphide ion; or (wherein R is OA and R1 is H) by reacting an isocyanate R2NCO with an alkanol <FORM:1026409/C2/3> and oxidizing the reaction product, e.g. Opponauer reaction. 1 -(N-phenyl-N1-ureido)-propanol-(2) is prepared from 2-hydroxypropylamine and PhNCO. Pharmaceutical compositions comprise compounds I (or their salts) and a pharmaceutically acceptable carrier therefor. The compositions, which possess analgetic, central nervous system depressant, antipyretic and anti-inflammatory activity may be formulated as tablets, dragees, suppositories or solutions for injection. |
