| 摘要 |
<p>The invention comprises sulphonamides of the formula <FORM:0976532/C1/1> and their acid addition salts, wherein A is a methylene or ethylene group and B is a nitrogen, oxygen or sulphur containing heterocyclic group attached to A through one of its carbon atoms, and the preparation of these compounds by reacting a 3-sulphamoyl-4-halo-benzoyl chloride with a carbinol B-A-OH and converting to a salt such as the hydrochloride, hydrobromide, sulphate, citrate, oxalate, tartrate, succinate, maleate, acetate, benzoate, hexahydrobenzoate, methanesulphanate, fumarate, gallate or hydroiodide, if desired. Examples describe tetra-hydrofuryl-, tetrahydropyranyl-, pyridyl-(21, 31 and 41)-, quinolyl-(21 and 41)- and thienyl -(21)-methyl esters and the 11-methyl-piperidyl-(21)-ethyl esters of the 3-sulphamoyl-4-chloro (and 4-fluoro)-benzoic acids. 3-Sulphamoyl-4-fluoro-benzoyl chloride used as a starting material is made by treating 4-fluorobenzoic acid with chlorosulphonic acid, treating the resulting 3-chlorosulphonyl-4-fluoro-benzoic acid with ammonia to give the corresponding 3-sulphamoyl compound and converting to the benzoyl chloride by reaction with thionyl chloride Pharmaceutical preparation having diuretic and saliuretic activity comprise the above compounds of the invention in admixture with an inert carrier.</p> |
