33263-43-3Relevant academic research and scientific papers
PROCESS FOR THE PREPARATION OF HIGHLY PURE TORSEMIDE
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Page/Page column 31-32, (2010/02/07)
The present invention provides a novel process for the preparation of highly pure torsemide [1] by reacting of 4-m-tolylamino-3-pyridinesulfonamide [2] with phenyl isopropylcarbamate in the presence of lithium base (F I, II). The present invention also provides a novel intermediate - torsemide lithium, also in hydrate or solvate form - which is a stable, solid compound, and may be simply isolated from the reaction mixture to give after acidification practically pure torsemide [1] without further purification steps.
Process for the preparation of chloropyridine sulphonic acid chlorides
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, (2008/06/13)
A process is disclosed for preparing chlorinated pyridinesulphonic acid chlorides of the general formula I from hydroxypyridine-sulphonic acids of the general formula II The process generally entails a) passing chlorine gas into a mixture of a hydroxypyridine-sulphonic acid and of phosphorus trichloride; b) heating the mixture of a) to temperatures of about 100 to about 120° C.; c) removing any phosphorus oxychloride formed and any excess phosphorus trichloride by distillation; d) taking up the residue with an organic solvent; and e) distilling the liquid phase in a vacuum, thereby obtaining the chlorinated pyridine-sulphonic acid chloride.
Chemistry and pharmacological properties of the pyridine-3-sulfonylurea derivative torasemide.
Delarge
, p. 144 - 150 (2007/10/02)
Out of a series of pyridine-3-sulfonylureas with diuretic activity torasemide (1-isopropyl-3- ([4-(3-methyl-phenylamino)pyridine]-3-sulfonyl)urea) has been proved to be one of the most active derivatives. In the rat, urinary volume and electrolyte excretions increased linearily with the logarithm of the dose, thus resembling the profile of a high ceiling diuretic. Experiments by oral and intravenous routes indicated that torasemide was equally potent both by oral and parenteral administration. Compared to furosemide, torasemide was 9-40 times more potent on weight basis in the rat. For the same natriuretic effect, however, potassium losses with torasemide were significantly less than with furosemide. The diuretic effect of torasemide lasted longer compared to that of furosemide. In accordance with the pharmacodynamic characteristics plasma elimination half-life of torasemide was about 1.5 h in the rat and bioavailability was nearly complete. Torasemide was 98-99% bound to plasma proteins. No in vitro interaction was found with the cumarine derivative warfarin.
