| 摘要 |
The invention comprises sulphonyl ureas of the formula <FORM:1031361/C2/1> and salts thereof, wherein R is a methyl or ethyl group and X and Y are each hydrogen, halogen, or a C1- 6 alkyl or alkoxy group and their preparation by (a) reacting a benzenesulphonyl isocyanate or a compound which reacts as an isocyanate such as a benzenesulphonyl carbamic ester, thiocarbamic ester or carbamic halide, or a benzenesulphonyl urea or N1-substituted urea such as an N1-acyl, N1-aryl, N1,N1-di-aryl or a N,N1-bis-benzenesulphonyl urea, with an N-alkyl-N-benzylhydrazine; (b) reacting a benzenesulphonamide with an N-alkyl-N-benzyl-imino-isocyanate or a compound which reacts as an isocyanate such as an N-alkyl-N-benzyl-hydrazino-N1-carboxylic acid ester, mono-thiocarboxylic ester or carboxylic acid halide or with a 1 - alkyl - 1 - benzyl - 4 - acyl - semicarbazide or 1,5 - dialkyl - 1,5 - dibenzyl carbazide or with a 1-alkyl-1-benzyl-semicarbazide which carries one or two aromatic substituents on the N4-atom, or (c) decomposing a 1-benzenesulphonyl - 3 - (N - alkyl - N - benzyl) - iminoparabani acid by hydrolysis, or a corresponding benzenesulphonyl-thiosemicarbazide by desulphuration with oxides or salts of heavy metals or with oxidizing agents such as hydrogen or sodium peroxide or nitrous acid. Pharmaceutical preparations having hypoglycaemic activity comprise the above compounds of the invention and a carrier, preferably in a form adapted to oral administration such as tablets. |
