| 摘要 |
<p>1,203,425. Benzenesulphonyl-ureas. FARBWERKE HOECHST A.G. 29 Nov., 1967 [29 Nov., 1966; 13 July, 1967], No. 54301/67. Heading C2C. Novel compounds I (including salts thereof) in which R represents a G 1-4 alkyl or C 1-4 alkenyl radical, X represents a hydrogen, fluorine, chlorine or bromine atom, or a C 1-4 alkyl or C 1-4 alkoxy radical in the 4- or 5-position relative to the carbamoyl group, and R<SP>1</SP> represents an endomethylene-cyclohexyl, endomethylene - cyclohexenyl, endoethylene - cyclohexyl or endoethylene-cyclohexenyl radical, are prepared utilizing standard methods. 1 -[4- (# - <2 -Methoxy-5 -chlorobenzamido> ethyl) - benzenesulphonyl} - 3 - (2,5 - endomethylene-cyclohexyl)-parabanic acid is obtained by the interaction of endomethylenecyclohexylparabanic acid and the appropriate benzenesulphonic acid chloride. N-[4-(#-<2-Methoxy-5-ahlorobenzamido>- ethyl) - benzenesulphinyl] - N<SP>1</SP> - (2,5 - endomethylene-cyclohexyl)-urea is prepared by reacting N - 2,5 - endomethylenecyclohexyl - urea with the appropriate benzenesulphinyl chloride. N - [4 - #-<2-Methoxy-5-chlorobenramido> - ethyl) - benzenesulphonyl] - N<SP>1</SP> - (2,5 - endomethylene-cyclohexyl)-thiourea, obtained by reacting the corresponding benzene sulphonamide with 2,5-endomethylenecyclohexyl isocyanate, is converted to N - [4 - # - < 2 - methoxy - 5 - chlorobenzamido> - ethyl) - benzenesulphonyl] - N<SP>1</SP>- (2,5 - endomethylenecyclohexyl) - isourea methyl ether by treatment with mercury oxide and ethanol in the presence of potassium carbonate followed by crystallization of the product from methanol. Pharmaceutical preparations having hypoglycemic activity contain as active ingredient compounds I; administration may be orally, e.g. in the form of a tablet. Reference has been directed by the Comptroller to Specification 1,080,705.</p> |
