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    • 2. 发明申请
    • A CRYSTALLINE SUBSTANCE OF CEFDITOREN PIVOXYL AND THE PRODUCTION OF THE SAME
    • CEFDITOREN PIVOXYL的晶体物质及其生产
    • WO1998012200A1
    • 1998-03-26
    • PCT/JP1997003340
    • 1997-09-19
    • MEIJI SEIKA KAISHA LTD.YASUI, KiyoshiONODERA, MasahiroSUKEGAWA, MasamichiWATANABE, TatsuoYAMAMOTO, YuichiMURAI, YasushiIINUMA, Katsuharu
    • MEIJI SEIKA KAISHA LTD.
    • C07D501/00
    • C07D501/00
    • As a novel substance is provided a new, crystalline substance of Cefditoren pivoxyl which has a high purity and an enhanced thermal stability on storage. This crystalline Cefditoren pivoxyl may be prepared by a process comprising a step of dissolving amorphous substance of Cefditoren pivoxyl in an anhydrous, first organic solvent capable of dissolving said amorphous substance well therein, and steps of replacing the first organic solvent component of the resulting solution by an anhydrous alkanol of 1 to 5 carbon atoms as a second organic solvent, in such a manner that the firstly prepared solution of Cefditoren pivoxyl in the first organic solvent is mixed with a volume of the alkanol and then is concentrated below 15 DEG C under reduced pressure, and so on. Thereby, the process proceeds so as to produce a solution containing 50 mg/ml to 250 mg/ml of Cefditoren pivoxyl dissolved in the alkanol alone. From the latter solution, crystals of Cefditoren pivoxyl are induced to deposit by addition of water at a temperature of 0 - 10 DEG C. The resulting admixture of the concentrated solution of Cefditoren pivoxyl in alkanol with added water and the deposited Cefditoren pivoxyl is then agitated 10 DEG C or below, to effect a complete crystallization of Cefditoren pivoxyl.
    • 作为一种新型物质,提供了一种具有高纯度和增加的储存热稳定性的新戊酸头孢托仑的结晶物质。 这种结晶的匹戊头孢托仑新戊酰基可以通过包括以下步骤的方法来制备,所述方法包括将新戊酰氧基新戊酰氧基的无定形物质溶解在能够很好地溶解所述无定形物质的无水的第一有机溶剂中,以及将所得溶液的第一有机溶剂组分置换为 将具有1至5个碳原子的无水链烷醇作为第二有机溶剂,使得将首次制备的在第一有机溶剂中的新戊酰氧基头孢托仑的溶液与一定体积的链烷醇混合,然后在15℃下浓缩, 压力等等。 由此,进行该处理,以产生溶解在单独的链烷醇中的含有50mg / ml至250mg / ml的新戊酰氧基甲脒基替他啶的溶液。 从后者的溶液中,通过在0-10℃的温度下加入水引发新戊酸头孢托仑的晶体沉淀。然后搅拌所得的新戊酰氧基甲基头孢地托仑在链烷醇中与加入的水的混合物和沉淀的新戊酰氧基新戊酰基 10℃或以下,以实现新戊酰氧基甲酰头孢托仑的完全结晶。