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.
本发明提供了一种新型方法,通过在
锂碱(F I,II)存在下,将
4-甲基苯胺基-3-
吡啶磺酰胺[2]与苯基异
丙基氨基甲酸酯反应,制备高纯度托瑟米特[1]。本发明还提供了一种新型中间体 - 托瑟米特
锂,也可以是
水合物或溶剂合物形式 - 这是一种稳定的固体化合物,可以简单地从反应混合物中分离出来,在酸化后得到几乎纯净的托瑟米特[1],无需进一步纯化步骤。