| 摘要 |
1,244,593. Sulphonyl-ureas and intermediates therefor. FARBENFABRIKEN BAYER A.G. 29 April, 1970 [29 April, 1969; 2 Dec., 1969], No. 20667/70. Heading C2C. Novel compounds I (including salts thereof) where R is an optionally unsaturated C 1 to C 10 aliphatic radical, or cycloalkyl or bi-, tri- or tetra-cycloalkyl radical optionally substituted by C 1 to C 4 alkyl, or corresponding rings in which R carries at the point of linkage to the adjacent -NH- a cyclic N-atom instead of a cyclic C-atom, as well as optionally alkyl-substitutedcycloalkylalkyl and - polycycloalkylalkyl radicals, R<SP>1</SP> and R<SP>11</SP> are H, halogens, alkyls which may be linked to comprise a fused ring, and/or phenyls optionally substituted by halogen or alkoxy, X is O, S or NR<SP>111</SP> (R<SP>111</SP> is H or alkyl, aryl or aralkyl, which may be substituted by halogen, alkyl, alkoxy or CF 3 ), Y and Z signify C 1 to C 3 alkylene which may be C 1 toC 4 alkyl substituted, or if one of Y or Z consists of at least two carbons, then the other can be a direct bond, are made according to standard methods, especially utilizing intermediate compounds II and III where A is, e.g. O-Methyl. The following starting materials and intermediates are also described and exemplified: 3 - acetyl - 2,3,4,5- tetrahydro - 1H - 3 - benzazepine - 7 - sulphonamide, 2,3,4,5 - tetrahydro - 1H - 3 - benzazepine- 7 - sulphonamide hydrochloride, 1 - acetyl - 1,2,3,4- tetrahydro - quinoline - 6 - sulphonamide and 1,2,3,4 - tetrahydro - quinoline - 6 - sulphonamide. Pharmaceutical preparations suitable for the oral treatment of diabetes, contain I as active ingredient.
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